Global Medicinal Chemistry & GPCR Summit

Las Vegas, USA   October 01-02, 2018

Scientific Program

Keynote Session:

Meetings International -  Conference Keynote Speaker Ravindra K Pandey photo

Ravindra K Pandey

Roswell Park Cancer Institute, USA

Title:  Epidermal growth factor receptor (EGFR) targeted multifunctional photosensitizers for bladder cancer imaging (Fluorescence and PET) and photodynamic therapy (PDT)

Biography:

Dr. Ravindra K Pandey is a Distinguished Member, Professor of Oncology and Director of Pharmaceutical Chemistry at Roswell Park Cancer Institute, Buffalo, NY, with extensive experience in drug design, drug delivery, molecular recognition, and tumor diagnostics. He has received several WNY inventor of the year awards, international award on heterocyclic chemistry, excellence in PDT award by ICPP, the American Chemical Society’s Jacob Schoelkopf award and China 1000 Talent Scientists Award for his contribution in translational research. Dr. Pandey is the Founder and Chief Scientific Officer (CSO) of Photolitec, LLC, a spin-off company of Roswell Park Cancer Institute. He has published around 300 research papers, review articles, book chapters, a book on cancer-imaging/therapy and several patents. 

 

Abstract:

This study describes the advantages of a multifunctional 124I-labeled [methyl-(1’-m-iodobenzyloxy)ethyl-3-devinyl-pyropheo phorbide-a (PET-ONCO) over the 18F-fluorodeoxy glucose (18F-FDG) for imaging bladder cancer by positron emission tomography (PET). As a non-radioactive analog, it can be used for fluorescence-guided PDT of bladder cancer. In our attempt to develop EGFR targeted multifunctional PS, an erlotinib moiety known for targeting EFGR was conjugated either at position-3 or at position-17 of the iodinated PS following the well-established Sonogashira cross coupling methodology. The comparative in vitro efficacy (cell uptake, intracellular localization and photosensitizing efficacy and EGFR target specificity) of the iodinated PS with and without an erlotinib moiety was investigated in UMUC-3 (EGFR positive) and T24 (EGFR low) cell lines. Among the parent PS and the erlotinib conjugated analogs, the PS containing the erlotinib moiety at position-17 showed best PET imaging and PDT efficacy. Interestingly, the position-3 erlotinib-PS conjugate was even less effective than the corresponding non-erlotinib analog. The position-17 erlotinib conjugate also showed higher in vivo uptake (determined by fluorescence), PET-imaging ability and PDT efficacy nude mice bearing UMUC3 tumors. 

 

Meetings International -  Conference Keynote Speaker Jinhwa Lee photo

Jinhwa Lee

1ST Biotherapeutics, Inc., South Korea

Title: Selective kinase inhibitors for the treatment of CNS disorders

Biography:

Jinhwa completed his PhD from the University of Alabama (1997) and Postdoctoral studies from Department of Chemistry and Chemical Biology, Harvard University (1997-1999). He was an investigator at the department of medicinal chemistry at GSK, Collegeville, PA (2000-2005), Director at Green Cross (2006-2011), Institut Pasteur Korea (2011-2014), and Handok (2015-2016) in Korea in the field of infectious disease, metabolic syndrome, cancer, and CNS. He has been the CTO of 1ST Biotherapeutics, Inc., a promising biotech in Korea since 2016. He has published more than 55 papers in reputed journals and has invented 18 US patents for drug discovery.

 

Abstract:

The kinase inhibitors have been utilized for the treatment of cancers since the discovery of the first drug, Imatinib. To date, there are over 40 kinase inhibitors approved by the US FDA, with a majority of these being small molecules. Despite the rapid growing development of kinase inhibitors for cancer, currently none of these agents are approved for CNS (central nervous system) diseases, mainly due to issues associated with CNS drug discovery. Protein kinases have been identified as potential therapeutic targets in neuronal cells and microglia. Many studies have suggested important roles of protein kinases in neuronal toxicity and microglial activation. Parkinson’s disease (PD) is the second most common neurodegenerative disorder. There are 7-10 million PD patients worldwide. So far there is no disease modifying therapy known. a-Synuclein and Lewy body pathology have been strongly implicated in PD and dementia with Lewy body. Abl (Abelson kinase, c-abl) is activated in various neurodegenerative conditions including AD, PD and ALS. Abl activation is sufficient to trigger neurodegeneration. Abl is activated by neuroinflammation, oxidative stress and mitochondrial dysfunction in neurons and microglia. Here the highlights of our drug discovery program toward the novel treatment of CNS disorders will be addressed along the line.

 

Oral Session 1:

  • Medicinal Chemistry |Anticancer Agents in Medicinal Chemistry | Herbal Plant Products and Nutraceutical | Organic Chemistry | Pharmacology
Speaker

Chair

Ravindra K Pandey

Roswell Park Cancer Institute, USA

Speaker

Co-Chair

Matteo Micucci

Bologna University, Italy

Meetings International -  Conference Keynote Speaker Matteo Micucci photo

Matteo Micucci

Scientist

Title: From natural products based research, new substances for the treatment of Candida sp infections: The case of Spirulina platensis

Biography:

Matteo Micucci has completed his PhD at Bologna University and he carries on his research focusing on Medicinal Chemisrty and Nutraceuticals. He was visiting scientist at the Research Laboratory of Medicinal Chemistry of De Montfort University, Leicester, UK. He was Visiting Scientist at University of Naples Federico II. He has published 28 papers in reputed journals and he has attended, as invited speaker and chairman national and international conferences. He won the International Awards Fides et Scientia. He is Science Adviser, in the field of Nutraceuticals, Integrative Medicines, at SEGRETERIA PARTICOLARE of a Senator of the Italian Republic.

 

Abstract:

Candidosis, caused by Candida spp., represents the most frequent mycosis of the oral cavity and of the vulvo-vaginal tract.1 Candidiasis is treated with anti-fungal agents including Nystatin, Miconazole, Itraconazole, Fluconazole and Amphotericin B. The efficacy of these drugs is limited by their side effects and antibiotics resistance. Several plants extract show antimicrobial activity and a good toxicological profile. The research based on natural products may lead to novel antifungal agents and nutraceuticals.In this work we investigated the chemical characterization of a Spirulina platensis water extract (SPE) and evaluated its effects towards uterine, esophageal and tracheal smooth muscle contractility, using in vitro biological assays. SPE antifungal effects were assessed against different Candida spp strains, isolated mostly from vaginal and oral swabs, by broth microdilution assay. HeLa, HEL 299 and VK2/E6E7 cells were used to investigate SPE citotoxicity. In SPE, phycobilins were found at the concentrations of 8.38 ± 0.89 mg/100 mg (Phycocyanin), 2.48 ± 0.60 mg/100 mg (Allo-Phycocyanin), 1.99 ± 0.62 mg/100 mg (Phycoerythrin); carotenoids and chlorophyll were detected at the concentrations of 1.97 ± 0.12 mg/g and 1.97 ± 0.12 mg/g, respectively. SPE did not affect uterine, esophageal and tracheal smooth muscle spontaneous contractility, while it exerted a concentration-dependent spasmolytic activity in KCl induced contraction, in uterus, suggesting a calcium antagonistic effect. SPE exerted antifungal properties (MIC: 0.125 ± 0.5 mg/ml), against all the Candida species with a fungicidal activity. Finally, in vitro cytotoxicity results of SPE on three different cell lines revealed a selectivity index between 2 and 16.

 

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Faizah Salah Aljohani

Assistant Professor

Title: Interaction of Eu(fod)3 with coordinated cyanide in an analogue of the sub-site of [FeFe]-hydrogenase

Biography:

Faizah Aljohani has completed his PhD from University of East Anglia. She worked under the supervision of Professor Christopher Pickett. Now, she works as Assistant Professor of Inorganic Chemistry at Taibah University in Saudi Arabia.

 

Abstract:

Second coordination sphere interactions of metal centres involving hydrogen bonding, ion-pairing or dipolar bonding can play an important role in determining the physical and chemical properties of molecular and biomolecular systems. For example, the redox potentials of cubane iron-sulfur clusters in a redox protein or enzyme can range between -700mV and -400mV versus the standard hydrogen electrode as a consequence of the nature  of the second-coordination sphere environment. Whilst this is largely explained in terms of hydrogen-bonding ionic, dipolar or other interactions may have a role in this. This study examines second coordination sphere interactions of coordinated cyanide in a model for the diiron subsite of [FeFe]-hydrogenase. The natural subsite in its protein environment catalyses hydrogen evolution (or uptake) at very fast rates ca 104 s-1 near the reversible potential of the H+ /1/2 H2 couple but such rates have yet to be attained in model systems. Controlling the electronic and geometric properties of synthetic diiron subsites by hydrogen bonding or other interactions might provide a means of attaining the turnover rates of the natural system. This work takes some first steps towards introducing second coordination sphere interactions to modify subsite properties. A metal Lewis acid Eu(fod)3 is shown to bridge to CN ligands in the model subsite to change its spectroscopic and electrochemical behavior.

 

Meetings International -  Conference Keynote Speaker Lamees S Al-Rasheed photo

Lamees S Al-Rasheed

Pharmacist

Title: Synthesis and antimicrobial activity of novel adamantylthiourea, isothiourea and related derivatives

Biography:

Lamees Alrasheed has her expertise working as outpatient, intravenous and in patient pharmacist at Prince Mohammed bin Abdulaziz Hospital, Riyadh, Saudi Arabia while obtaining her master’s degree in medicinal chemistry.

 

 

Abstract:

The incorporation of an adamantyl moiety into several molecules results in compounds with relatively high lipophilicity, which in turn can modify the biological availability of these molecules. Beyond increasing partition coefficients, the adamantyl group positively modulates the therapeutic index of many experimental compounds, through a variety of mechanisms. Several adamantane derivatives have long been known for their diverse biological properties, mainly as antiviral, antibacterial and antifungal. In addition, thiourea and isothiourea nucleus were reported to constitute the pharmacologically active moiety of several compounds. On these bases, new series of 1-adamantyl derivatives, in which the adamantyl moiety was covalently conjugated to arylthiourea or 4-Thiazolidinone moieties have been synthesized as potential bioactive agents. The reaction of 1-adamantylamine with various aryl isothiocyanates yielded the corresponding 1-(adamantan-1-yl)-3-arylthiourea derivatives (A). The reaction of the thioureas (A) with various arylmethyl bromides and ethyl bromoacetate, in acetone, in the presence of potassium carbonate yielded the corresponding (Z)-3-(adamantan-1-yl)-1-aryl-S-(benzyl or substituted benzyl)-isothioureas (B) and ethyl 2-[(Z)-1-(adamantan-1-yl)-3-arylisothioureido]acetates (C). The 3-(adamantan-1-yl)-2-aryliminothiazolidin-4-ones (D) were obtained by cyclization of the ethyl 2-[(Z)-1-(adamantan-1-yl)-3-arylisothioureido] acetates (C) via prolonged heating with sodium acetate in ethanol. The structures of the compounds (A-D) were confirmed by analytical and spectral data and single crystal X-ray diffraction. Compounds (A-D) were tested for in vitro activities against a panel of Gram-positive and Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans, several derivatives produced good or moderate activities particularly against tested Gram-positive bacteria. In this investigation, 27 new target compounds were prepared, 15 of them displayed potent antibacterial activity.

 

Meetings International -  Conference Keynote Speaker Plato A Magriotis photo

Plato A Magriotis

Associate Professor

Title: Documentation of the first catalytic enantioselective gilman-speeter synthesis of β-Lactams

Biography:

Since 2006, Plato A. Magriotis, Ph.D., is an Associate Professor of Medicinal Chemistry in the Department of Pharmacy at the University of Patras in Greece and a Research Affiliate with the Department of Chemistry at New York University. Magriotis received his Ph.D. in Chemical Biology with Professor Francis Johnson at Stony Brook University in 1983 and did Postdoctoral work at Harvard University with Nobel Laureate Professor E. J. Corey. His career started at West Virginia University and continued at Merck & Co. as well as New York University in the U.S., prior to his return to Greece. Magriotis’ research program focuses on the development of new methodology for the synthesis of relevant pharmacophores applied in drug discovery.

 

Abstract:

In recent years, organocatalysts have dominated the field of asymmetric organic synthesis due to their ability to catalyze a variety of fundamentally important transformations. One example is the Staudinger synthesis of β-lactams which continue to provide unique opportunities for the design and synthesis of new derivatives with unprecedented biological profiles other than antibacterial activity. In fact, during the last two decades medicinal chemists have convincingly demonstrated that structural modifications of monocyclic β-lactams (monobactams) is an effective protocol for the discovery of new derivatives with novel pharmacological profiles. This lecture will cover recent progress that has been made in asymmetric organocatalytic Staudinger synthesis of β-lactams since the inaugural and pioneering investigations by Lectka and coworkers around the turn of the century,1 as well as our own efforts toward the development of a novel Gilman-Speeter process for the catalytic enantioselective synthesis of β-lactams.   

 

Meetings International -  Conference Keynote Speaker Mahesh Pal photo

Mahesh Pal

Principal Scientist

Title: Antimicrobial activity of sonchus arvensis

Biography:

Mahesh Pal received PhD degree in Plant Natural Product Chemistry in 1998 from CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow, India and Postdoctoral studies from State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany Kunming, China. He is serving as Principal Scientist in Phytochemistry Division at CSIR-National Botanical Research Institute, a premier Government organization, Lucknow, India. He has published more than 65 research papers in reputed journals and has been serving as an editorial board member of ten reputed journals. Currently he is working on isolation and identification of bio-molecules for anticancer, antidiabetic and antimicrobial activity from Indian medicinal Plants.

 

Abstract:

Sonchus arvensis (Asteraceae) is an annual plant that is easy to grow in rainy and sunshine areas, such as on riverbanks, ridges of rice field. S. arvensis is one of the medicinal herbs used in traditional medicines, in which the leaf extract was used as a diuretic, lithotriptic and anti urolithiasis agent; also indicated for fever, poisoning and swelling or abscess.  The plant is valued as a delicious and nutritional herb and has been used for the treatment of caked breasts, asthma, coughs, and other chest complaints and for calming the nerves. The fresh root of S. arvensis crushed and hydrodistilled for extraction of essential oil. The chemical composition of the essential oil obtained from the root of S. arvensis with yield of 0.18% (w/v), was analyzed by the GC and GC-MS. A total of 15 components, representing 97.2% of the oil, were identified. The oil composition is dominated by the presence of aromatic hydrocarbons accounting for 43.55% while as sesquiterpenes constitute 15.66% of the total oil composition. The principal components found was 9, 10-Dithiaanthacene constitute 43.55% of the total volatile constituents. Main identified constituents were β-Patchoulene (4.80%), Caryophyllene oxide (9.93%), Caryophyllene (4.24%), and β- Eudesmol (4.98%). The antibacterial activity of the volatile oils tested was more pronounced against Gram- positive than against Gram-negative bacteria. In conclusion, to the best of our knowledge the essential oil composition and its antimicrobial activity of the roots of S. arvensis is the first report. 

Meetings International -  Conference Keynote Speaker Sigal Eilat Adar photo

Sigal Eilat Adar

Head of a second degree program in Healthy and Active Lifestyle Education

Title: Nutritional assessment at a girls’ orphanage in Trincomalee, Sri Lanka according to length of stay

Biography:

Sigal Eilat-Adar is a registered nutritionist and an epidemiologist. She did her postdoctoral project studying the epidemiology of the association between the diet of American Indians and Native Alaskans and cardiovascular disease (CVD). Since then, her expertise is in the evaluation of nutritional public health and she is passionate about improving health and well-being. She is the head of a second degree program in Healthy and Active Lifestyle Education at The Academic College at Wingate, Wingate Institute, Israel.  For the past three decades she has worked as a clinical nutritionist in the Israeli Health Services, and she leads the Israel position statement on nutritional guidelines for prevention and treatment of CVD. In the last few years, she has volunteered in various communities around the world, sharing her knowledge and treatment skills.

 

Abstract:

The civil war in 1983 and the 2004 tsunami in the island country of Sri Lanka both created a large number of health problems, particularly in coastal areas of the country. According to the Demographic Health Survey (DHS) for Sri Lanka, in the period 2006-2007 17.3% of children under five were found to be stunted, 14.7% were suffering from malnutrition, and 21.1% were underweight.  The current study summarizes the nutritional assessment of the children at Grace Girls’ Home (GRACE), an orphanage in the city of Trincomalee in northeast Sri Lanka, according to their length of stay at the orphanage. Thirty-one girls aged 5-19 years old were in the care of the institution at the time of the survey. Height-for-age, weight-for-age, and BMI-for-age z-scores (HAZ, WAZ, and BMIZ, respectively) were calculated based on anthropometric measurements. Time at GRACE did not vary according to age at entrance.  BMIZ was significantly higher in girls who stayed longer at GRACE –  -0.69±0.82 in girls staying up to five years as compared to -0.15±0.44 in those staying over five years (P=0.001). There was a positive association between the length of stay at the institution and BMIZ, regardless of current age (r=0.54 P=0.006), which disappeared after adjustment for age at entrance (r=0.33 P=0.121). However, age at entrance by itself was not associated with the BMIZ score for age (r=-0.14 P=0.505). These results show that the length of stay in a secured place is associated with better growth, as expressed by BMIZ. From this small, specific group one can conclude that orphans residing in an orphanage benefit from a healthy weight gain and nutritional outcomes.

 

Meetings International -  Conference Keynote Speaker Xiu Qiu photo

Xiu Qiu

Director

Title: Gestational weight gain rate and adverse perinatal outcomes: Results from a Chinese birth cohort study

Biography:

Xiu Qiu has completed her PhD of Maternal, Children and Adolescents Health from the Chinese Center for Disease Control and Prevention, Beijing, China. She is the Director and a Principle Investigator in Born in Guangzhou Cohort Study. She has broad research interests in the epidemiology of maternal and child health, including gestational diabetes, preterm birth, fetal growth, child development. She has coauthored of over 30 publications including Lancet, Environmental Health Perspectives, European Journal of Epidemiology, GigaScience, Ebiomedicine etc.

 

Abstract:

Objective: To explore relationships between gestational weight gain rate (GWGR) and adverse perinatal outcomes in a large population from a developing country.Methods: Prospective data from 17181 pregnant women in the Born in Guangzhou Cohort Study, China was included. GWGR (kg/week) was calculated by dividing the total GWG (kg) by gestational weeks at which the maternal weight at delivery was measured. Stratified by pre-pregnancy BMI sub-groups (<18.5, 18.5-24.9, and ≥25kg/m2), associations between GWGR and preterm birth, cesarean delivery and neonatal asphyxia (Apgar score at 1 minute ≤7) were examined using logistic regression.

Results: The proportions of underweight, normal weight, and overweight/obese prior to pregnancy were 23.8%, 70.0%, and 6.2%. The mean GWGRs of these three groups were 379.79g/week, 367.71g/week, 301.78 g/week, respectively. Among underweight mothers, high weight gain rate (>mean+1 SD) was associated with an increased risk of preterm birth (OR [95%CI], 1.59 [1.01-2.52]) and caesarean section (1.49[1.21-1.83]) compared to adequate GWGR (mean±1SD). For mothers with normal weight, low weight gain rate (

Conclusion: Both high and low weight gain rate was associated with adverse perinatal outcomes.

 

Keynote Session:

Meetings International -  Conference Keynote Speaker Mahesh Pal photo

Mahesh Pal

CSIR-Central Institute of Medicinal and Aromatic Plants, India

Title: New source of andrographolide having potential biological activities

Biography:

Mahesh Pal received PhD degree in Plant Natural Product Chemistry in 1998 from CSIR-Central Institute of Medicinal and Aromatic Plants, Lucknow, India and Postdoctoral studies from State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany Kunming, China. He is serving as Principal Scientist in Phytochemistry Division at CSIR-National Botanical Research Institute, a premier Government organization, Lucknow, India. He has published more than 65 research papers in reputed journals and has been serving as an editorial board member of ten reputed journals. Currently he is working on isolation and identification of bio-molecules for anticancer, antidiabetic and antimicrobial activity from Indian medicinal Plants.

 

Abstract:

Cancer has been considered to be very dreadful disease. Holmskioldia sanguinea is a large climbing shrub found in the Himalayas at an altitude of 5,000 ft and preliminary investigation showed the excellent yield of andrographolide and subjected for the anticancer activity. Protective effect of Holmskioldia sanguinea leaf ethanolic extract has been investigated against Ehrlich ascites carcinoma (EAC) and Daltons ascites lymphoma (DAL) in Swiss albino mice and to evaluate the possible mechanism of action. The enzymatic antioxidant status was studied on tumour bearing mice, which shows the potential of the compound to possess significant free radical scavenging property and revealed significant tumour regression and prolonged survival time. The isolated bioactive molecule andrographolide from Holmskioldia sanguinea yields (2.5%) in subject to HPTLC/HPLC analysis. The cellular defence system constituting the superoxide dismutase, catalyses was enhanced whereby the lipid peroxidation content was restricted to a larger extent. The Holmskioldia sanguinea is a new source of andrographolide and demonstrated the potency in treatment of cancer.     

 

Oral Session 1:

  • Medicinal Chemistry | Anticancer Agents in Medicinal Chemistry |Herbal Plant Products and Nutraceutical | Organic Chemistry | Pharmacology
Speaker

Chair

M Constantine Samaan

McMaster University, Canada

Speaker

Co-Chair

Ravindra K Pandey

Roswell Park Cancer Institute, USA

Meetings International -  Conference Keynote Speaker Sadaf Shakoo photo

Sadaf Shakoo

Lecturer

Title: Qualitative, quantitative screening and proximate analysis of commercially available food colorants tartrazine and curcumin: Before and after addition to feed

Biography:

Sadaf Shakoor has her expertise in food, nutrition and food services for the maintenance of normal daily food intake. She is basically a Lecturer in the field of nutrition at University of Agriculture, Faisalabad, She have experience as nutritionist, both in hospital and education institutions. Pakistan. She is pursuing PhD in the subject of Nutritional Sciences at University Putra Malaysia. She is dealing with food color specially tartrazine and curcumin in her PhD research project. She has skills and knowledge necessary to be effective at promoting overall improved health.

 

Abstract:

Statement of the problem: Current many study mentioned about severe health issues from constant employ of coloring agents through food. So, it is important to understand the consequences by the use of food color in food products by worldwide. Food color depicted as an interesting ingredient for food industry mainly due to their appearance imparting into food products. The synthetic food color such as tartrazine derived from coal tar whereas natural, curcumin are obtained from the medicinal plants Curcuma longa or plant parts. Methodology & Theoretical Orientation: Proximate analysis, qualitative and quantitative phytochemicals screening of food colors and feed containing food colors were analyzed in aqueous, ethanolic and methanolic extracts. Purpose of this study is to evaluate qualitative and quantitative screening of commercially available food colorants tartrazine and curcumin and their effect on nutritive value of rats feed. Feeds were prepared by addition of low (9.6mg/kg; 3.85mg/kg) and 10 times high dosage (96mg/kg; 38.5mg/kg of tartrazine and curcumin (Control, low tartrazine, high tartrazine, low curcumin, high curcumin feed). Findings: Results revealed that slight variation was seen in moisture (27.1 % in LT), protein (21.87% in HT), fat (4.18% in LT), ash (7.26% in HT), and fiber (3.85% in HC) content of all five feed. The qualitative analysis reflect the presences of alkaloids, anthraquinone, carbohydrates, coumarines, flavonoids, glycosides, resins, saponins and tannins in the extracts of feed. The quantitative analysis exposed the maximum concentration of carbohydrates (3691mg/dl) flavonoids (403µg/ml), phenols (114µg/ml) in methanolic extract of HC, alkaloids (508mg/dl) in methanolic extract of control feed and tannins (297g/ml) in methanolic extract of LC feed. Conclusion & Significance: Food coloring agent incorporation affects nutritive value of feed, showed presence of some anti-nutritional substances i.e. tannins and saponins. Whereas, it is necessary to fruitfully apply tartrazine and curcumin during processing and formation of food stuffs.

 

Title: Impact of delivery vehicles in tumor-specificity, imaging and therapy of multifunctional agents

Biography:

 

Dr. Ravindra K Pandey is a Distinguished Member, Professor of Oncology and Director of Pharmaceutical Chemistry at Roswell Park Cancer Institute, Buffalo, NY, with extensive experience in drug design, drug delivery, molecular recognition, and tumor diagnostics. He has received several WNY inventor of the year awards, international award on heterocyclic chemistry, excellence in PDT award by ICPP, the A​merican Chemical Society’s Jacob Schoelkopf award and China 1000 Talent Scientists Award for his contribution in translational research. Dr. Pandey is the Founder and Chief Scientific Officer (CSO) of Photolitec, LLC, a spin-off company of Roswell Park Cancer Institute. He has published around 300 research papers, review articles, book chapters, a book on cancer-imaging/therapy and holds several patents. 
 

Abstract:

The poor water solubility of most of the porphyrin-based photosensitizers (PS) causes significant problems in clinical development, and the choice of a suitable formulation with limited toxicity is an important step in drug development. In recent years, a wide variety of formulating systems such as Tween 60, cremophor, liposomes, microcapsules, microspheres, nanoparticles, nanocrystals and polymers are being explored. However, reproducibility, biocompatibility, premature degradation or inactivation within the systemic circulation and toxicity at higher doses are the problems associated with some of these formulations. Therefore, it becomes necessary to investigate the toxicity (including organ toxicity) of these formulating agent(s) before their use in drug formulation. We have shown that the nature of delivery vehicles makes a significant difference in tumor-uptake and biological efficacy. The limitations and advantages of certain vehicles in developing multifunctional agents will be presented.

 

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Matteo Micucci

Scientist

Title:  Polyphenols in Obesity: new perspectives from a network based approach

Biography:

Matteo Micucci has completed his PhD from University of Bologna and Postdoctoral Studies from Department of Pharmacy and Biotechnology, University of Bologna. He has published more than 25 papers in reputed journals and has been serving as an editorial board member of several conferences.

 

 

Abstract:

Obesity is a multifactorial pathology due to an excessive accumulation of fats in adipose tissue and peripheral organs. Also oxidative stress and inflammation exert a central role in the onset and progression of this pathology. Other events occurring along with obesity consist of the alteration of vascular and gastrointenstinal smooth muscle contractility, oxidative stress mechanisms impairment, liver alterations, increases of serum lipids. Medical therapies recommended for obesity include a wide spectrum of pharmaceutical molecules, such as, among others, sibutramine, orlistat, lorcaserin, phentermine, liraglutide.  In face of the severe side effects of these drugs, natural products and vegetal extracts are now preferably used for the management of obesity, overweight and related disorders. In this study, we evaluated the effects of a natural chestnut wood extract (NCWE) against different parameters altered in obesity, including body weight, food intake, liver functionality and histology, liver phase I and II enzymes, gastrointestinal oxidative stress, serum lipids and cytokines. For this purpose 120 male Sprague-Dawley rats were used and divided into 4 groups: Regular diet (RD) fed rats, High Fat Diet (HFD) fed rats, RD fed rats administred with NCWE (20 mg/Kg), HFD fed rats administered NCWE (20 mg/Kg). The parameters were assessed after one week of treatment, two weeks of treatment and three weeks of treatment. HFD rats underwent significant modifications of most measured parameters that were inhibited by NCWE treatment. The data support the potential use of NCWE for the management of obesity and related disorders.

 

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Rick Falkenberg

Managing Partner

Title: Evaluation of an advance oxidation system in controlling healthcare-associated infections on various surfaces

Biography:

Rick Falkenberg received his PhD in Microbiology and Immunology from the University of California San Diego further identifying the correlation between hexose-monophosphate shunt, glycolytic system and fermentation-type in specific lactobacilli strains. He is recognized as a process authority and is well established with FDA, USDA FSIS and CODEX requirements, specifically high acid, low-acid, acidified foods, non-thermal applications as we low moisture foods. His group provides consulting and technical support to the processed food, spice, nut and nutraceutical industries in the areas of pasteurization and sterilization process validation, implementation of shelf stable food products, co-packer identification/evaluation and commercial production transfer.

 

Abstract:

The effectiveness of reactive oxygen species (ROS) generating airPHX equipment for reducing bacterial populations of Clostridium difficile, Methicillin Resistant Staphylococcus aureus (mRSA) and Pseudomonas aeruginosa on three (3) common contact  surfaces;  stainless  steel  (Austenitic  316),  plastic  (PVC)  and  linoleum (floor  tile)  were  studied.  Antimicrobial  resistant  pathogens  pose  an  ongoing and increasing challenge to hospitals because they cause healthcare-associated infections  (HAIs)  during  clinical  treatment  of  patients.  Coupons  of  stainless steel, plastic and linoleum were inoculated with each organism placed inside an experimental chamber were continuously treated with ROS for eight different hour increments from an airPHX advanced oxidation generator. ROS levels were continuously monitored prior to removing coupons for microbiological testing. Control coupon were similarly placed in the chamber and held at environmental conditions to determine natural decay of microbial populations through time. Stainless steel coupon results after 0.5 h of ROS treatment Clostridium difficile Methicillin Resistant Staphylococcus aureus (mRSA) and Pseudomonas aeruginosa saw a 4.21-log, 4.42-log and 4.26-log destruction respectively. After 12 h exposure, these same organisms yielded a 6.87-log, 7.17-log and 7.71-log reduction, respectively. The other contact surfaces, plastic and linoleum displayed similar log reduction. These findings reveal that ROS treatment using the airPHX unit significantly reduces these three HAI’s on common health care contact materials to > 4.2-log destruction after a 0.5 h exposure.

 

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Mohsen Khalid

Consultant

Title: Fractalkine as an inflammatory marker in obese subject

Biography:

Prof. Dr. Mohsen Khalid has graduated from faculty of medicine Cairo University in November 1980. He has completed his Master degree in Internal Medicine May 1986, and then he completed his Medical Doctorate in Internal Medicine November 2003. He is a consultant of Diabetes and Endocrinology in the Egyptian National Institute of Diabetes and Endocrinology. He has published more than 20 papers in reputed journals. The research interest of Prof. Dr. Mohsen Khalid is Genetics of Diabetes, diabetic complications and how to assist diabetic patients to live a good life with life style modification and medical treatment

 

Abstract:

Title: Multicomponent reaction to synthesize 3,5-dicyano-6-sulfanylpyridine and its derivatives

Biography:

Mayasim Amer Almotairi is pursuing his bachelor degree of general chemistry from King Abdulaziz University.

 

Abstract:

Multicomponent reactions (MCR) have gained popularity over the past few decades in the world of chemistry.  (MCR) is a chemical reaction where 3 or more compounds react together to produce a one product. The concept of privileged medicinal scaffolds was originally introduced by Merck researchers, during the course of their work on benzodiazepines, recently acting as a guiding principle in modern drug discovery.  Privileged scaffolds generally consist of a rigid ring structure such as a heterocyclic ring. 3,5-Dicyanopyridines are an important privileged heterocyclic scaffold. In our research, we explored the methodology to synthesize 4-aryl-6-sulfanylpyridine derivatives by MCR. The derivatives of 4-phenylpyridine are reported to show excellent biological activities.  A three-component reaction of 4-anisaldehyde, malonitrile, and NaSH produced a very important intermediate-2-amino-3,5-dicyano-6-mercapto-4-(4-methoxyphenyl)-pyridine. Alkylation reaction on sulfur of this intermediate will result in various 3,5-dicyano-6-sulfanyl pyridine products as desired. All products were characterized by 1H NMR and 13C NMR spectroscopy. 
 
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Ioannis Grigoriadis

Scientific Director

Title: Glybatomaq312317b: A hyper-ligand playing a role in angiogenesis, controlling endothelial cell motility and invasion

Biography:

Ioannis Grigoriadis has completed his Pharmacist D at the age of 24 years from Aristotle University of Thessaloniki. He is the Scientific Director of Biogenea Pharmaceuticals Ltd, a premier biotechnology personalized cancer vaccination service organization. He has published more than 20 papers in reputed journals and has been serving as an editorial board member of reputeon the collection, processing, cryopreservation and cGMP production for solely autologous use of cellular therapeutical solutions from blood (bone marrow, peripheral blood, cord blood) or blood compounds for human use on stem cell expansion technologies, which were created in the research laboratories of NASA (National Aeronautics and Space Administration), cGMP production of advanced medicinal products (1394/2007/ C) for solely autologous use from skin, dental pulp, cord tissue) and also in preclinical-research phase: on certified genetic analyses in collaboration with Ε International Referral Centers-on copyright protection according to the American and/or European Copyright Agency.

 

Abstract:

Free energy perturbation (FEP) ab initio quantum mechanics (QM) methods were developed for treating the solute molecules and molecular mechanics (MM) for treating the surroundings. Like earlier results using AM1 semi empirical QMs, the ab initio QM/MM-based FEP method was shown to accurately calculate relative solvation free energies for a diverse set of small molecules that differ significantly in structure, aromaticity, hydrogen bonding potential, and electron density.  Accuracy was similar to or better than conventional FEP methods. Together with PML, Nuclear autoantigen Sp-100 tumor suppressor is a major constituent of the PML bodies, a subnuclear organelle involved in a large number of physiological processes including cell growth, differentiation and apoptosis. Functions as a transcriptional coactivator of ETS1 and ETS2 according to PubMed:11909962. Under certain conditions, it may also act as a corepressor of ETS1 preventing its binding to DNA according to PubMed:15247905. Through the regulation of ETS1 it may play a role in angiogenesis, controlling endothelial cell motility and invasion. Through interaction with the MRN complex it may be involved in the regulation of telomeres lengthening. May also regulate TP53-mediated transcription and through CASP8AP2, regulate FAS-mediated apoptosis. Also plays a role in infection by viruses, including human cytomegalovirus and Epstein-Barr virus, through mechanisms that may involve chromatin and/or transcriptional regulation. The QM/MM-based methods eliminate the need for time-consuming development of MM force field parameters, which are frequently required for drug-like molecules containing structural motifs not adequately described by MM. Future automation of the method and parallelization of the code for Linux 128/256/512 clusters is expected to enhance the speed and increase its use for drug design and lead optimization. We introduce Glybatomaq, an Ab initio Systematic Parametrization of Polarizable Force Fields from Quantum Chemistry mechanics-based free energy perturbation method for calculating relative solvation free energies for systematic force field optimization with the ability to parametrize a wide variety of functional forms using flexible combinations of reference data. Amber FFs for proteins have been continually improved in recent years and a detailed discussion of the various changes is beyond the scope of this review. Significant revisions have been published, with particular emphasis on important dihedral angles. Development of the Drude polarizable FF in CHARMM (58) started in 2001 and the capability to simulate the Drude model is now included in NAMD (59), ChemShell QM/MM (60) and the OpenMM suite of utilities for GPUs (61). Development of the force field first involved implementation of the appropriate integrators to allow computationally efficient extended Langrangian MD simulations (62). We outline several important challenges in force field development and how they are addressed in ForceBalance, and present an example calculation where these methods are applied to develop a highly accurate polarizable novel Nano-ligand targeted to the Nuclear autoantigen Sp-100, sp|P23497|568-592, KRWQQRGRKANTRPLKRRRKRGPRI, P23497 playing a role in angiogenesis, controlling endothelial cell motility and invasion through the regulation of the ETS1, CASP8AP2 and FAS-mediated apoptosis.