Synthesis and biological activity of new 2,4,6-trisubstituted triazines as potential phosphoinositide 3-kinase inhibitors

被引:4
作者
Xin, Minhang [1 ]
Wang, Hui-Yan [1 ]
Zhang, Hao [1 ]
Shen, Ying [1 ]
Zhang, San-Qi [1 ]
机构
[1] Xi An Jiao Tong Univ, Hlth Sci Ctr, Dept Med Chem, Sch Pharm, Xian 710061, Shaanxi, Peoples R China
关键词
anticancer; antiproliferative effects; PI3K inhibitor; synthesis; triazine derivatives; ANTITUMOR-ACTIVITY EVALUATION; KINASE INHIBITOR; PI3K; CANCER; TARGET; IDENTIFICATION; DERIVATIVES; DISCOVERY; PATHWAY; DESIGN;
D O I
10.1177/1747519820904844
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Twenty-five novel 2,4,6-trisubstituted triazines were synthesized and biologically evaluated. Most of the compounds synthesized showed good antiproliferative activity against HCT-116 and MCF-7. CompoundsB18andB19showed the best antiproliferative activity. Further study showedB18andB19inhibited four phosphoinositide 3-kinase isoforms and mammalian target of rapamycin with good potency. These results demonstrate that 2,4,6-trisubstituted triazines are potentially useful phosphoinositide 3-kinase inhibitors for the development of new anticancer drugs.
引用
收藏
页码:393 / 402
页数:10
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