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.

Abstract

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

MeSH terms

  • 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

Substances

  • Antineoplastic Agents
  • Biphenyl Compounds
  • Receptors, Vasoactive Intestinal Polypeptide, Type I
  • Small Molecule Libraries
  • Thiophenes