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Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of advanced solid tumors

Hao‐Yue Xiang, Xiang Wang, Yanhong Chen, Xi Zhang, Cun Tan, Yi Wang, Yi Su, Zhiwei Gao, Xiaoyan Chen, Bing Xiong, Zhaobing Gao, Yi Chen, Jian Ding, Linghua Meng, Chunhao Yang

2020European Journal of Medicinal Chemistry31 citationsDOIOpen Access PDF

Topics & Concepts

ChemistryCarbamateTrifluoromethylStereochemistryOrally activeMedicinal chemistryOrganic chemistryIn vitroBiochemistryAlkylPI3K/AKT/mTOR signaling in cancerSynthesis and biological activityQuinazolinone synthesis and applications
Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of advanced solid tumors | Litcius