Format

Send to

Choose Destination
J Comb Chem. 2007 Jan-Feb;9(1):107-14.

Design and synthesis of an array of selective androgen receptor modulators.

Author information

1
GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA. ryan.p.trump@gsk.com

Abstract

We describe the design, using shape comparison and fast docking computer algorithms, and rapid parallel synthesis of a 1300 member array based on GSK7721, a 4-aminobenzonitrile androgen receptor (AR) antagonist identified by focused screening of the GSK compound collection. The array yielded 352 submicromolar and 17 subnanomolar AR agonists as measured by a cell-based reporter gene functional assay. The rapid synthesis of a large number of active compounds provided valuable information in the optimization of AR modulators, which may be useful in treating androgen deficiency in aging males.

PMID:
17206838
DOI:
10.1021/cc060096e
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for American Chemical Society
Loading ...
Support Center