Identification and optimization of small molecule antagonists of vasoactive intestinal peptide receptor-1 (VIPR1)

Bioorg Med Chem Lett. 2012 Mar 15;22(6):2287-90. doi: 10.1016/j.bmcl.2012.01.082. Epub 2012 Feb 2.

¹ Early Discovery Chemistry, Bristol-Myers Squibb Co., Princeton, NJ 08543-4000, USA. lalgudi.harikrishnan@bms.com

Abstract

Identification, synthesis and structure-activity relationship of small-molecule VIPR1 antagonists encompassing two chemical series are described.

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology
Biphenyl Compounds / chemical synthesis*
Biphenyl Compounds / pharmacology
Cell Line, Tumor
Drug Screening Assays, Antitumor
High-Throughput Screening Assays
Humans
Receptors, Vasoactive Intestinal Polypeptide, Type I / antagonists & inhibitors*
Receptors, Vasoactive Intestinal Polypeptide, Type I / metabolism
Small Molecule Libraries
Structure-Activity Relationship
Thiophenes / chemical synthesis*
Thiophenes / pharmacology