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Discovery of pyrazole-thiophene derivatives as highly Potent, orally active Akt inhibitors. 2019
Wenhu Zhan, and
Jinxin Che, and
Lei Xu, and
Yizhe Wu, and
Xiaobei Hu, and
Yubo Zhou, and
Gang Cheng, and
Yongzhou Hu, and
Xiaowu Dong, and
Jia Li
ZJU-ENS Joint Laboratory of Medicinal Chemistry, Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, Hangzhou Institute of Innovative Medicine, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, PR China.
A series of pyrazole-thiophene derivatives exhibiting good Akt inhibitory activities were obtained on the basis of conformational restriction strategy, leading to the discovery of compound 1d and 1o which showed excellent in vitro antitumor effect against a variety of hematologic cancer cells and their potential of inducing apoptosis, blocking the cell cycles at S phase and significantly inhibiting the phosphorylation of downstream biomarkers of Akt kinase of cancer cells. Amongst, compound 1o also exhibited good PK profiles and inhibited about 40% tumor growth in MM1S xenograft model. Compound 1o might be a potential candidate for further development.
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