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2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain.

Authors
  • Young, Jonathan R
  • Huang, Song X
  • Walsh, Thomas F
  • Wyvratt, Matthew J
  • Yang, Yi Tien
  • Yudkovitz, Joel B
  • Cui, Jisong
  • Mount, George R
  • Ren, Rena Ning
  • Wu, Tsuei Ju
  • Shen, Xiaolan
  • Lyons, Kathryn A
  • Mao, An Hua
  • Carlin, Josephine R
  • Karanam, Bindhu V
  • Vincent, Stella H
  • Cheng, Kang
  • Goulet, Mark T
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry Letters
Publisher
Elsevier
Publication Date
Mar 11, 2002
Volume
12
Issue
5
Pages
827–832
Identifiers
PMID: 11859012
Source
Medline
License
Unknown

Abstract

A series of 2-arylindoles containing novel heteroaromatic substituents on the tryptamine tether, based on compound 1, was prepared and evaluated for their ability to act as gonadotropin releasing hormone (GnRH) antagonists. Successful modifications of 1 included chain length variation (reduction) and replacement of the pyridine with heteroaromatic groups. These alterations culminated in the discovery of compound 27kk which had excellent in vitro potency and oral efficacy in rodents.

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