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Bioorg Med Chem Lett. 2012 Jan 15;22(2):1208-12. doi: 10.1016/j.bmcl.2011.11.080. Epub 2011 Nov 30.

New thiazole carboxamides as potent inhibitors of Akt kinases.

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Key Laboratory of Regenerative Biology and Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, No. 190 Kaiyuan Avenue, Science Park, Guangzhou 510530, China; Graduate School of Chinese Academy of Sciences, # 19 Yuquan Road, Beijing 100049, China.


A new series of 2-substituted thiazole carboxamides were identified as potent pan inhibitors against all three isoforms of Akt (Akt1, Akt2 and Akt3) by systematic optimization of weak screening hit N-(1-amino-3-phenylpropan-2-yl)-2-phenylthiazole-5-carboxamide (1). One of the most potent compounds, 5m, inhibited the kinase activities of Akt1, Akt2 and Akt3 with IC(50) values of 25, 196 and 24nM, respectively. The compound also potently inhibited the phosphorylation of downstream MDM2 and GSK3β proteins, and displayed strongly antiproliferative activity in prostate cancer cells. The inhibitors might serve as lead compounds for further development of novel effective anticancer agents.

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