Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 180, Issue -, Pages 72-85Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.07.017
Keywords
Pyrazole-thiophene derivatives; Akt inhibitor; Antitumor
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Funding
- National Natural Science Foundation of China
- National Major Scientific and Technological Special Project for Significant New Drugs Development
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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. (C) 2019 Elsevier Masson SAS. All rights reserved.
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