期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 10, 页码 4728-4739出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm300204j
关键词
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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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