TY - JOUR
T1 - Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl) quinoxalines as PI3Kα inhibitors
AU - Wu, Peng
AU - Su, Yi
AU - Liu, Xiaowen
AU - Zhang, Lei
AU - Ye, Yong
AU - Xu, Jianchao
AU - Weng, Shaoyu
AU - Li, Yani
AU - Liu, Tao
AU - Huang, Shufang
AU - Yang, Bo
AU - He, Qiaojun
AU - Hu, Yongzhou
PY - 2011/11
Y1 - 2011/11
N2 - 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).
AB - 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).
KW - 2-Arylamino-3-(arylsulfonyl)quinoxaline
KW - Cytotoxicity
KW - PI3K
KW - PI3Kα
UR - http://www.scopus.com/inward/record.url?scp=80054880978&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=80054880978&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2011.09.015
DO - 10.1016/j.ejmech.2011.09.015
M3 - Article
C2 - 21945250
AN - SCOPUS:80054880978
SN - 0223-5234
VL - 46
SP - 5540
EP - 5548
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
IS - 11
ER -