Archived: 1st Winter Conference
on Medicinal & Biooriganic Chemistry

January 29th - February 2nd 1995

Steamboat Springs Resort, Colorado

Agenda

Sunday, January 29th 1995

Monsanto/NSERC Symposium on Stereoselective Synthesis in Medicinal Chemistry

Program Chair: Dr Victor Snieckus, University of Waterloo

Dr Victor Snieckus University of Waterloo

Overview: Recent Methods in Peptidomimetic Assemblage

Dr Michael Kahn Molecumetics

Peptide Secondary Structure Mimetics: Recent Advances and Future Challenges

Dr Dale Kempf Abbott Laboratories

Peptidomimetics in Drug Design: Orakky Bioavailable Inhibitors of HIV Protease

Dr Peter Beak University of Illinois

Asymetric Syntheses: Highly Enantioselective Carbon-carbon Bond Formations Vased on Asymmetric Deprotonation of Carbamate Esters

Dr Dieter Hoppe Wilhelms-Universität Münster

Enantio- and Diastereoselective Syntheses of Aminoalcohols and Related Compounds via Asymmetric Deprotonation of Carbamate Esters

Dr Amos Smith University of Pennsylvania

The Total Syntheses of Rapamycin and Dimethoxyrapamycin

Dr Stephen Martin University of Texas

Applications of Stereoselective Synthesis in Bioorganic Chemistry

Dr Larry Overman University of California Irvine

New Stereocontrolled Methods for Ring Formation

Dr A.G.M Barrett Imperial College

Recent Advances in the Synthesis of Bioactive Natural Products

Monday, January 30th 1995

Molecular Mechanism of Signal Transduction

Program Chair: Dr Grant Krafft, Northwestern University Medical Center

Dr Grant Krafft Northwestern University Medical Center

Cellular Modes of Signal Transduction: An Overview

Dr Gary Johnson University of Colorado

Integration of Signal Transduction Pathways Regulated By Heterotrimeric G-Proteins and Tyrosine Kinases

Dr David Goeddel Tularik Inc.

Signalling via TNFα Receptor

Dr Heidi Hamm University Illinois-Chicago

G-Proteins in Signal Transduction

Dr Tona Gilmer Glaxo Inc.

SH2 Domains and Inhibitors

Dr James Woodgett Ontario Cancer Center

Nuclear Signal Transduction

Dr David Robertson Ligand Pharmaceuticals

Steroid Superfamily Receptors: Prototypic Ligand-Gated Transcription Factors

Tuesday, January 31st 1995

KEYNOTE | “Molecular Probes for Steroid Receptors: Structure, Modeling and Medical Imaging”

Program Chair: Prof. John A. Katzenellenbogen, University of Illinois

General Oral Papers | Session I

Program Chair: Mike Rafferty

Dr John McCall Upjohn Co.

Tirilizad Mesylate: A Novel and Effective Treatment for Acute Neurologic Disorders, Mechanism of Action and Pharmacology

Dr Bruce A. Lefker Pfizer

Rational Design of Non-peptide Renin Inhibitors

Dr Wanye Broulliette University of Alabama

Structure-Based Inhibitors of Influenza Viral Neuraminidase. Development of a Benzoic Acid Lead

Dr R.P. Iyer Hybridon Inc.

Bioreversible Analogs of Oligonucleotides: Stereospecific Conversion of S-alkyl Phosphorothiolates to Phosphorothioates

Dr Carston Wagner University of Minnesota

Amino Acid Phosphoramidates of Antiviral Nucleosides Exhibit High Potency and Low Toxicity

Dr Robert Volkmann Pfizer

Discovery of a Novel Pos-Translational Isomerization of Ser46 in ω-Aga-IVB and ω-Aga-IVC, Calcium Channel Toxins Isolated from the Agelenopsis Aperta Spider

Robert Moore University of Kansas

Photoaffinity Probes of DNA Polymerase Structure and Function

Dr Karen Lackey Glaxo

Rigid Analogs of Camptothecin as DNA Topoisomerase Inhibitors

General Oral Papers | Session II

Program Chair: Dan Flynn

Dr Jeffrey Aubé University of Kansas

Linker Design for β-Turn Formation

Dr G.G. Weingarten Glaxo Inc.

Stereo-Control in the Convergent Synthesis of Chiral Carbocyclic Nucleoside Analogues

Dr Raymond Funk Pennsylvania State University

Synthetic Approaches to Taxol and Analogs

Dr Vincent Kalish Agouron

Structure-Based Drug Design and Optimization of HIV Protease Inhibitors

Dr Andrea Leone-Bay Emisphere Inc.

Microsphere Formation and Drug Delivery in a Series of Derivatized Amino Acids

Dr Bruce Dorsey Merck

Synthesis and Evaluation of Pyridyl Analogs of L-735,524: Potent HIV Protease Inhibitors

Dr Bryan H. Norman Lilly

Wortmannin Analogs are Potent Inhibitors of Photsphatidylinositol-3-Kinase

Dr David Reitz Searle

Novel 1,2-Diarylcyclopentenes are Potent, Selective, and Orally Active COX-2 Inhibitors

Evening Poster Program

1. Dr Norman Abood Searle

Conformationally Restricted, Nonpeptide Fibrinogen Receptor Antagonists: Design and Synthesis of Orally Active, Long Acting Inhibitors of GPIIB/IIIA Mediated Platelet Aggregation

2. Dr Daniel P. Becker Searle

Enantioslective Synthesis of the Dual 5-HT4/5-HT3 Serotonergic Agent SC-52491

3. Dr G.S. Bisacchi Bristol-Myers Squibb

Aminodiol Inhibitors of HIV Protease: Modifications at P2 which Enhance Potency

4. Dr Wayne Broulliette UAB

A Conformationally Defined 6-S-trans-Retinoic Acid Isomer with Chemoprotective Activity and Toxicity Comparable to Retinoic Acid

5. Dr Karl-Heinz Czaplinski University of Kansas

Predicting the Activites of Taxol Analogues Using CoMFA

6. Dr Raymond Funk Pennsylvania State University

Photochemical Cycloaromatization Reactions of ortho-Dialkynylarenes. New DNA Photocleaving Agents

7. Dr Shelly Glase Parke-Davis

Synthesis and Characterization of Fruan Dihydrofuran Analogs of the Dopamine D3 Ligand 7-OH-DPAT

8. Dr Julia Heerding Sphinx

Synthesis and Biological Activities of Balanol Analogs as Protein Kinase C Inhibitors: A Study of Carboxylic Acid Replacementts

9. Dr Michael Hoemann University of Kansas

Synthesis of 13-epi- Taxol via Transannular Delivery of a Borohydride Reagent

10. Dr R.P. Iyer Hybridon Inc.

Synthesis of [35S] 3H-1,2- BEnzodithiole-3-one-1,1- Dioxide: Application in the Preparation of Site-specifically 35S-Labeled Oligonucleotides

11. Dr E. Jon Jacobsen Upjohn

High Affinity Partial Agonist Imidazo [1,5-a]quinoxaline Piperazine Ureas at the GABAa/Benzodiazepine Receptor Complex

12. Dr Kevin Koch Pfizer

The Design, Synthesis, and Pharmacology of the Potent, Orally Active LTB4 Antagonist, CP-105696

13. Brian Kornberg Parke-Davis

Design and Synthesis of Phosphorus and Hydroxamate Inhibitors of Endothelin Converting Enzyme

14. Ms. Ke Li University of Kansas

Photoprobes of Nucleic Acid Polymerase Substrate Blinding Sites

15. Dr Amparo Lago Smithkline Beecham

The Rational Design and Synthesis of Potent, Nonpeptide Endothelin Receptor Antagonists

16. Dr Juan I. Luengo Smithkline Beecham

Selective Manipulation of the Pampamycin Effector Domain: Synthesis and Evaluation of C-7 Derivatives and the X-ray Crystal Structures of their Complexes with FKBP12

17. Dr Thomas C. Malone Park Davis

Preparation and Evaluation of Substituted 1,4,7,8,9,10-Hexahydropyrido [4,3-fjquinoxaline-2,3-diones as AMPA Receptor Antagonists

18. Dr Sanjay Menon University of Kansas

Classical Hansch Analysis and Comparative Molecular Field Analysis (CoMFA) of the Phenylethanolamine N-Methyltransferase (PNMT) Inhibitory Activity of Benzylamines

19. Dr Bryan H. Norman Lilly

Stereoselective Synthesis of Novel Methylene Ether Dipeptide Isosteres

20. Dr David Oare Genentech

Spatially Diverse Libraries for Pharmaceutical Lead Discovery

21. Dr John Proudfoot Boehringer-Ingelheim

2-Aryl Substituted Dipyridodiazeoinones are Potent Inhibitors of HIV-1 Reverse Transcriptase and Possess Activity Against the Y181C Mutant Enzyme

22. Dr Michael Reuman Sterling-Winthrop

Synthesis and Binding Affinity of 2,3,3a,4,9,9a-Hexahydro-(Iminomethano)-1H-Benz[f]indenes. Ligands for the PCP site of the NMDA Receptor.

23. Dr Karen Romines Upjohn

Cycloalkylpyranones: A New Template for the Design of Potent, Non-Peptidic HIV Protease Inhibitors

24. Dr David Rotella Cephalon

Carboline and Carbazole Derivatives of K252C as Potential Small Molecule Neurotrophic Agents

25. Dr Malcolm Scott R.W.Johnson

Novel Antipsychotics with Unique D2/5-HT1a Affinity and Minimal Extrapyramisal Side-Effect Liability

26. Dr Thomas Shih Merck

An Improved Method for Synthesizing C24,C25-Substituted Avermectins

27. Niels Skærbæk Royal Danish College of Pharmacy

Equilibrium in Bromomethylation of 5-Cyclopropyl-3-Hydroxyisoxazole

28. Dr John Tulinsky Upjohn

A Novel Assymetric Synthesis of Atropisomeric 6-Aryl Pyrazinores via an Unusual Chirality Transfer Process

29. Dr John A. Wendt University of Kansas

Toward the Total Synthesis of (-)-Sparteine

30. Dr Christine Yoakim BioMega

Novel Substituted Pipecolinic Amide Dertivatives as HIV Protease Inhibitors

31. Dr Dennis Zimmerman Eli Lilly

Molecular Modelling of the Phenylpiperidine Antagonist LY-255582 with Other Opioids Suggests a Model of Antagonist and Agonist Binding to Opioid Receptors

Wednesday, February 1st 1995

Recent Advances in Enzyme Inhibitor Discovery

Program Chair: Dr Daniel Rich, University of Wisconsin

Dr Daniel Rich University of Wisconsin

Overview: Recent Advances in Enzyme Inhibitor Discovery

Dr Petr Kuzmic University of Wisconsin

Novel Enzyme Kinetic Mechanisms

Dr Dinesh Patel Affymax

Application of Combinatorial Chemistry to the Determination of Novel Inhibitors for Proteases

Dr Patrick Lam DuPont-Merck

Structure-based Design of HIV Protease Inhibitors

Dr William Ripka Corvas Pharmaceuticals

Thrombin and Factor Xa Inhibitors

Dr Daniel Getman Searle

Rational Design of HIV Protease Inhibitors

Dr Bradley Tait Park-Davis

HIV Protease Inhibitors: Nonpeptide Leads from Compound Collections

Dr Alan Chrusciel Upjohn

Novel HIV Protease Inhibitor Templates

Thursday, February 2nd 1995

The Re-emergence of Natural Products as a Source of New Therapeutics

Program Chair: Dr Lester Mitscher, University of Kansas

Dr Lester Mitscher University of Kansas

Introduction, Historical Considerations, and Overview

Dr Sidney Hecht University of Virginia

Higher Plants with Anticancer and Antifungal Activity

Dr John Cardellina NCI

Higher Plants with Antiviral and Other Activities

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