| Literature DB >> 22554206 |
Chuangxing Guo1, Indrawan McAlpine, Junhu Zhang, Daniel D Knighton, Susan Kephart, M Catherine Johnson, Haitao Li, Djamal Bouzida, Anle Yang, Liming Dong, Joseph Marakovits, Jayashree Tikhe, Paul Richardson, Lisa C Guo, Robert Kania, Martin P Edwards, Eugenia Kraynov, James Christensen, Joseph Piraino, Joseph Lee, Eleanor Dagostino, Christine Del-Carmen, Ya-Li Deng, Tod Smeal, Brion W Murray.
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.Entities:
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Year: 2012 PMID： 22554206 DOI： 10.1021/jm300204j
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446