ACS Medicinal Chemistry Letters p. 543 - 547 (2015)
Update date:2022-07-29
Topics:
Li, Yingjun
Cheng, Huimin
Zhang, Zhang
Zhuang, Xiaoxi
Luo, Jinfeng
Long, Huoyou
Zhou, Yang
Xu, Yong
Taghipouran, Rana
Li, Dan
Patterson, Adam
Smaill, Jeff
Tu, Zhengchao
Wu, Donghai
Ren, Xiaomei
Ding, Ke
A series of N-(3-ethynyl-2,4-difluorophenyl)sulfonamides were identified as new selective Raf inhibitors. The compounds potently inhibit B-RafV600E with low nanomolar IC50 values and exhibit excellent target specificity in a selectivity profiling investigation against 468 kinases. They strongly suppress proliferation of a panel of human cancer cell lines and patient-derived melanoma cells with B-RafV600E mutation while being significantly less potent to the cells with B-RafWT. The compounds also display favorable pharmacokinetic properties with a preferred example (3s) demonstrating significant in vivo antitumor efficacy in a xenograft mouse model of B-RafV600E mutated Colo205 human colorectal cancer cells, supporting it as a promising lead compound for further anticancer drug discovery.
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