New thiazole carboxamides as potent inhibitors of Akt kinases

S Chang, Z Zhang, X Zhuang, J Luo, X Cao, H Li…

文献索引：Chang, Shaohua; Zhang, Zhang; Zhuang, Xiaoxi; Luo, Jinfeng; Cao, Xianwen; Li, Honglin; Tu, Zhengchao; Lu, Xiaoyun; Ren, Xiaomei; Ding, Ke Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 2 p. 1208 - 1212

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被引用次数: 20

摘要

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 IC50 values of 25, 196 and 24nM, respectively. The compound also potently inhibited the ...

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Discovery of GSK1070916, a potent and selective inhibitor of...

[Adams, Nicholas D.; Adams, Jerry L.; Burgess, Joelle L.; Chaudhari, Amita M.; Copeland, Robert A.; Donatelli, Carla A.; Drewry, David H.; Fisher, Kelly E.; Hamajima, Toshihiro; Hardwicke, Mary Ann; Huffman, William F.; Koretke-Brown, Kristin K.; Lai, Zhihong V.; McDonald, Octerloney B.; Nakamura, Hiroko; Newlander, Ken A.; Oleykowski, Catherine A.; Parrish, Cynthia A.; Patrick, Denis R.; Plant, Ramona; Sarpong, Martha A.; Sasaki, Kosuke; Schmidt, Stanley J.; Silva, Domingos J.; Sutton, David; Tang, Jun; Thompson, Christine S.; Tummino, Peter J.; Wang, Jamin C.; Xiang, Hong; Yang, Jingsong; Dhanak, Dashyant Journal of Medicinal Chemistry, 2010 , vol. 53, # 10 p. 3973 - 4001]