Discovery of pyrroloaminopyrazoles as novel PAK inhibitors

Journal of Medicinal Chemistry
Chuangxing GuoBrion 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.

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Apr 8, 2014·Cancer Letters·Byung Jun RyuSangYoun Park
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