2-(3-丁炔酰胺基苯基)苯并噻唑衍生物作为抗肿瘤剂的合成与生物学评价

[Synthesis and biological evaluation of 2-(3-butynoicamidophenyl) benzothiazole derivatives as antitumor agents].

作者信息

Yin Gui-Lin, Li Yan, Tang Ke, Jin Xiao-Feng, Chen Xiao-Guang, Li Li, Feng Zhi-Qiang

出版信息

Yao Xue Xue Bao. 2014 Jun;49(6):888-95.

PMID:25212037

Abstract

A series of 2-(3-butynoicamidophenyl)benzothiazole derivatives were synthesized starting from 4-fluoro-3-nitrobenzoic acid. Structures of all the synthesized compounds were confirmed by 1H NMR and HR-MS. Their antitumor activities against human tumor cells lines (HCT116, Mia-PaCa2, U87-MG, A549, NCI-H1975) were evaluated by MTT assay. The results revealed that most of the synthesized compounds showed potent activities against HCT116, Mia-PaCa2, U87-MG tumor cells lines. Particularly, compounds 14c and 14h exhibited better activity with IC50 values of 1 x 10(-8) mol x L(-1) against U87-MG and HCT116 respectively. The structure-activity relationship of compounds was also discussed preliminarily.

摘要

以4-氟-3-硝基苯甲酸为起始原料，合成了一系列2-(3-丁炔酰胺基苯基)苯并噻唑衍生物。所有合成化合物的结构均通过1H NMR和HR-MS得以确证。采用MTT法评估了它们对人肿瘤细胞系（HCT116、Mia-PaCa2、U87-MG、A549、NCI-H1975）的抗肿瘤活性。结果表明，大多数合成化合物对HCT116、Mia-PaCa2、U87-MG肿瘤细胞系表现出较强活性。特别地，化合物14c和14h表现出更好的活性，对U87-MG和HCT116的IC50值分别为1×10(-8) mol·L(-1)。还初步探讨了化合物的构效关系。