115351-23-0Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel (E)-α- benzylsulfonyl chalcone derivatives as potential BRAF inhibitors
Li, Qing-Shan,Li, Cui-Yun,Lu, Xiang,Zhang, Hui,Zhu, Hai-Liang
experimental part, p. 288 - 295 (2012/07/14)
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 BRAF V600E inhibitor. Based on its structure, a series of novel (E)-α-benzylsulfonyl chalcone derivatives (13-40) were designed and synthesized. Compound 38 exhibited the most potent inhibitory activity with an IC50 value of 0.17 μM for BRAFV600E and GI50 value of 0.52 μM for mutant BRAF-dependent cells. The results of cell based pERK activity and cellular selectivity suggested that those compounds could selectively inhibit proliferation of mutant BRAF-dependent melanoma cell line through inhibition of oncogenic BRAF.
