Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists

Zhiqiang Guo; Dongpei Wu; Yun-Fei Zhu; Fabio C Tucci; Collin F Regan; Martin W Rowbottom; R Scott Struthers; Qiu Xie; Shelby Reijmers; Susan K Sullivan; Yang Sai; Chen Chen

doi:10.1016/j.bmcl.2005.05.038

Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists

Bioorg Med Chem Lett. 2005 Aug 15;15(16):3685-90. doi: 10.1016/j.bmcl.2005.05.038.

Authors

Zhiqiang Guo¹, Dongpei Wu, Yun-Fei Zhu, Fabio C Tucci, Collin F Regan, Martin W Rowbottom, R Scott Struthers, Qiu Xie, Shelby Reijmers, Susan K Sullivan, Yang Sai, Chen Chen

Affiliation

¹ Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. zguo@neurocrine.com

PMID: 15951171
DOI: 10.1016/j.bmcl.2005.05.038

Abstract

SAR studies of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists resulted in potent compounds. The best compound from the series had a binding affinity of 2 nM.

MeSH terms

Drug Evaluation, Preclinical
Humans
Molecular Structure
Receptors, LHRH / antagonists & inhibitors*
Structure-Activity Relationship
Triazines / chemical synthesis
Triazines / chemistry
Triazines / pharmacology*

Substances

Receptors, LHRH
Triazines