Journal article
Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Kα inhibitors
ZJU-ENS Joint laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.1
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).
| Language: | English |
|---|---|
| Year: | 2011 |
| Pages: | 5540-5548 |
| ISSN: | 17683254 and 02235234 |
| Types: | Journal article |
| DOI: | 10.1016/j.ejmech.2011.09.015 |
2-Arylamino-3-(arylsulfonyl)quinoxaline Cell Line, Tumor Chemistry Techniques, Synthetic Class Ia Phosphatidylinositol 3-Kinase Cytotoxicity Drug Evaluation, Preclinical Enzyme Inhibitors Humans Inhibitory Concentration 50 Models, Molecular PI3K PI3Kα Phosphoinositide-3 Kinase Inhibitors Protein Conformation Quinoxalines Structure-Activity Relationship
