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

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

  • Eur J Med Chem. 2011 Nov;46(11):5540-8. doi: 10.1016/j.ejmech.2011.09.015.
Peng Wu 1,  Yi Su,  Xiaowen Liu,  Lei Zhang,  Yong Ye,  Jianchao Xu,  Shaoyu Weng,  Yani Li,  Tao Liu,  Shufang Huang,  Bo Yang,  Qiaojun He,  Yongzhou Hu
Affiliations

Affiliation

  • 1 ZJU-ENS Joint laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
PMID: 21945250 DOI: 10.1016/j.ejmech.2011.09.015
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 IC(50): 0.07 μM) displayed the most potent cellular activities (IC(50) values of 0.14 μM, 0.07 μM, 0.95 μM and 0.05 μM against PC3, A549, HCT116 and HL 60, respectively).

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