Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Kα inhibitors

Peng Wu, Yi Su, Xiaowen Liu, Lei Zhang, Yong Ye, Jianchao Xu, Shaoyu Weng, Yani Li, Tao Liu, Shufang Huang, Bo Yang, Qiaojun He, Yongzhou Hu

Research output: Contribution to journalJournal articleResearchpeer-review

Abstract

A series of novel 2-arylamino-3-(arylsulfonyl)quinoxalines was synthesized through a newly developed approach. All synthesized target compounds were screened for their cytotoxicities against cancer cell lines including PC3, A549, HCT116, HL60 and KB. Representative compounds with favorable cytotoxicities were tested for their PI3Kα inhibitory activities. Among the synthesized target compounds, 17 (PI3Kα IC50: 0.07 μM) displayed the most potent cellular activities (IC50 values of 0.14 μM, 0.07 μM, 0.95 μM and 0.05 μM against PC3, A549, HCT116 and HL 60, respectively).
Original languageEnglish
JournalEuropean Journal of Medicinal Chemistry
Volume46
Issue number11
Pages (from-to)5540–5548
ISSN0223-5234
DOIs
Publication statusPublished - 2011
Externally publishedYes

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