Literature DB >> 21945250

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

Peng Wu1, Yi Su, Xiaowen Liu, Lei Zhang, Yong Ye, Jianchao Xu, Shaoyu Weng, Yani Li, Tao Liu, Shufang Huang, Bo Yang, Qiaojun He, Yongzhou Hu.   

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).
Copyright © 2011 Elsevier Masson SAS. All rights reserved.

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Year:  2011        PMID: 21945250     DOI: 10.1016/j.ejmech.2011.09.015

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  4 in total

Review 1.  Recent syntheses of PI3K/Akt/mTOR signaling pathway inhibitors.

Authors:  Mark E Welker; George Kulik
Journal:  Bioorg Med Chem       Date:  2013-05-09       Impact factor: 3.641

Review 2.  Recent development of ATP-competitive small molecule phosphatidylinostitol-3-kinase inhibitors as anticancer agents.

Authors:  Yu Liu; Wen-Zhu Wan; Yan Li; Guan-Lian Zhou; Xin-Guang Liu
Journal:  Oncotarget       Date:  2017-01-24

Review 3.  Recent advances in the transition-metal-free synthesis of quinoxalines.

Authors:  Biplob Borah; L Raju Chowhan
Journal:  RSC Adv       Date:  2021-11-19       Impact factor: 4.036

4.  Identification of novel piperazinylquinoxaline derivatives as potent phosphoinositide 3-kinase (PI3K) inhibitors.

Authors:  Peng Wu; Yi Su; Xianghong Guan; Xiaowen Liu; Jiankang Zhang; Xiaowu Dong; Wenhai Huang; Yongzhou Hu
Journal:  PLoS One       Date:  2012-08-14       Impact factor: 3.240

  4 in total

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