Article
Discovery and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations.
Bioorganic & medicinal chemistry letters - 15 Jun 2022
Liu Xile, Zhang Lu, Wan Haiwen, Zhu Zhenzhen, Jin Jing, Qin Yuxin, Mao Weifeng, Yan Kang, Fang Douglas, Jiang Wen, Hu Lihong, Chen Jinhua, Chen Kevin, Chen Shuhui, Li Jian, Zhao Shuyong, Zheng Shansong, Zhang Long, Ding Charles Z
Abstract excerpt
ALK gene rearrangements are oncogenic drivers in approximately 5% of NSCLC. Crizotinib, a first generation ALK inhibitor, is widely prescribed for ALK-positive NSCLC in clinic. Resistance to crizotinib and other ALK inhibitors has been problematic. Addressing resistance, here we describe discovery and development of a novel, proprietary spirocyclic diamine-substituted aryl phosphine oxide series of inhibitors,...
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