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

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).

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Wu P,Su Y,Liu X,Zhang L,Ye Y,Xu J,Weng S,Li Y,Liu T,Huang S,Yang B,He Q,Hu Y

doi

10.1016/j.ejmech.2011.09.015

subject

Has Abstract

pub_date

2011-11-01 00:00:00

pages

5540-8

issue

11

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(11)00675-1

journal_volume

46

pub_type

杂志文章

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