Synthesis and characterization of new s-triazine bearing benzimidazole and benzothiazole derivatives as anticancer agents

被引:32
作者
Kumar, G. Jagadeesh [1 ,3 ]
Kumar, S. Naveen [1 ]
Thummuri, Dinesh [3 ]
Adari, Lavanya Bindu Sree [3 ]
Naidu, V. G. M. [3 ]
Srinivas, Kolupula [3 ]
Rao, V. Jayathirtha [1 ,2 ,3 ]
机构
[1] CSIR, Indian Inst Chem Technol, Crop Protect Chem Div, Hyderabad 500607, Andhra Pradesh, India
[2] CSIR, Indian Inst Chem Technol, AcSIR IICT, Hyderabad 500607, Andhra Pradesh, India
[3] NIPER, Hyderabad 500037, Andhra Pradesh, India
关键词
s-Triazine benzimidazole derivatives; s-Triazine benzothiazole derivatives; Anticancer activity; Structure-activity relationships; ANTIBACTERIAL ACTIVITY; INHIBITORS; POTENT; DISCOVERY; MTOR; TARGET; OPTIMIZATION; SERIES;
D O I
10.1007/s00044-015-1430-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Two new series of s-triazine derivatives appended with benzimidazole (15a-h) and benzothiazole derivatives (16a-h) are synthesized, and structure-activity relationships on anticancer activity of these 15a-h and 16a-h were probed. In vitro inhibitory activity against the growth of six cancer cell lines, viz., MCF-7, MDAMB-231, PC-3, DU-145, HT-29 and HGC-27 was evaluated for synthesized analogues. Among the two series of compounds, derivatives containing benzimidazole scaffold were found to be relatively potent over benzothiazole analogues. In accordance with our previous observation, within benzimidazole derivatives, tri-substituted s-triazine derivatives were found to be more potent over di-substituted derivatives irrespective of cell lines. Structure-activity relationships provided useful insights into these classes of compounds and paved the way to design novel analogues with more potency.
引用
收藏
页码:3991 / 4001
页数:11
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