Format

Send to

Choose Destination
J Med Chem. 2012 May 24;55(10):4728-39. doi: 10.1021/jm300204j. Epub 2012 May 14.

Discovery of pyrroloaminopyrazoles as novel PAK inhibitors.

Author information

1
Pfizer Global Research and Development, 10770 Science Center Drive, San Diego, California 92121, United States. alexguo01@gmail.com

Abstract

The P21-activated kinases (PAK) are emerging antitumor therapeutic targets. In this paper, we describe the discovery of potent PAK inhibitors guided by structure-based drug design. In addition, the efflux of the pyrrolopyrazole series was effectively reduced by applying multiple medicinal chemistry strategies, leading to a series of PAK inhibitors that are orally active in inhibiting tumor growth in vivo.

PMID:
22554206
DOI:
10.1021/jm300204j
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for American Chemical Society
Loading ...
Support Center