Design, synthesis and biological evaluation of novel (E)-α-benzylsulfonyl chalcone derivatives as potential BRAF inhibitors

QS Li, CY Li, X Lu, H Zhang, HL Zhu

Index: Li, Qing-Shan; Li, Cui-Yun; Lu, Xiang; Zhang, Hui; Zhu, Hai-Liang European Journal of Medicinal Chemistry, 2012 , vol. 50, p. 288 - 295

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Citation Number: 18

Abstract

Activating mutations in the BRAF serine/threonine kinase are found in more than 70% of human melanomas,> 90% of which are BRAFV600E. It provides new therapeutic opportunities in malignant melanoma. In silico and in vitro screening of our compound collection has identified Hit 2 as BRAFV600E inhibitor. Based on its structure, a series of novel (E)-α-benzylsulfonyl chalcone derivatives (13–40) were designed and synthesized. ...