Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists

Authors
Lin, P Parikh, M Lo, JL Yang, YT Cheng, K Smith, RG Fisher, MH Wyvratt, MJ Goulet, MT
Citation
P. Lin et al., Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists, BIOORG MED, 11(8), 2001, pp. 1077-1080
Citations number
5
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
8
Year of publication
2001
Pages
1077 - 1080
Database
ISI
SICI code
0960-894X(20010423)11:8<1077:HDO2AG>2.0.ZU;2-8
Abstract
A series of heterocyclic 2-(3,5-dimethylphenyl)tryptamine derivatives was p repared and evaluated on a rat gonadotropin releasing hormone receptor assa y. The carbon tether length and heterocyclic ring attached to the amino gro up of 2-(3,5-dimethylphenyl)tryptamine were varied. Several of these deriva tives were potent GnRH antagonists with the most potent compound having an IC50 of 16nM. (C) 2001 Elsevier Science Ltd. All rights reserved.