Symposium to Honor Dr. Istvan Lengyel
Saturday, November 9, 2013 from 1:00 PM to 5:00 PM (PST)
New York, NY
1:00pm Welcoming Remarks.
1:15pm William Pitts, R.Ph., Ph.D., Senior Principal Scientist Immunology Chemistry at Bristol-Myers Squibb.
Title: Molecular Modeling, Synthesis & Medicinal Chemistry.
Abstract: This presentation will focus on the interplay between molecular modeling and synthetic organic chemistry to aid medicinal chemistry efforts. Syntheses of target molecules and relevant pharmacology in the areas of HIV protease, MEK, IMPDH, MMP-13, and IKappa B Kinase will be discussed.
2:00pm Dr. Peter Gorycki, Ph.D., Director, Biotransformation at GlaxoSmithKline
2:45pm Coffee Break
3:15pm Tony Taldone, Ph.D., Senior Research Scientist at Memorial Sloan-Kettering
Title: Discovery and Development of Purine-scaffold Hsp90 inhibitors for the Treatment of Cancer. Abstract: Heat shock protein 90 (Hsp90) is a molecular chaperone exploited by cancer cells to aid in their survival. The recognition of Hsp90 as a critical facilitator for oncogene addiction and survival of cancer cells has opened a promising new niche for cancer treatment. The serendipitous discovery that the broad spectrum anticancer activity of the natural products geldanamycin (GM) and radicicol (RD) was a result of inhibition of Hsp90 resulted in the development of improved derivatives of these natural products. One of these was 17-AAG, a closely related analog of GM, and was in fact the first Hsp90 inhibitor to enter the clinic. However, GM and its analogs suffer from poor "drug-like" properties and this served as a strong impetus for the development of novel synthetic Hsp90 inhibitors. One class to exhibit enhanced potency and improved pharmacokinetic properties is the purine-scaffold. A number of small-molecule Hsp90 inhibitors based on the purine-scaffold are currently being evaluated in clinical trials for cancer. Here, I will discuss their initial discovery and development into potential anticancer agents.
4:00pm Victor Cesare, Ph.D., Professor at St. John’s University
Title: The Chemistry of a-Lactam According to Dr. Istvan Lengyel
Abstract: Dr. Lengyel was a pioneer and leader in the field of a-lactam chemistry for over 40 years. This talk will highlight is contributions starting with his Ph.D. work at MIT and concluding with his 10 year collaboration with this speaker.
5:00pm Dinner for students, speakers, guests Location: TBA