Synthesis and Antiproliferative Activity of NewN-Acylhydrazone Derivatives Containing Benzothiazole and Indole Based Moiety

被引：19
作者：
Liu, Kai [1 ]
Ding, Yangyang [1 ]
Kang, Congmin [1 ]
机构：
[1] Qingdao Univ Sci & Technol, Coll Chem Engn, Qingdao 266042, Peoples R China
来源：
PHARMACEUTICAL CHEMISTRY JOURNAL | 2020年 / 54卷 / 04期
关键词：
synthesis; N-acylhydrazone; benzothiazole; indole based moiety; antiproliferative activity; BIOLOGICAL EVALUATION; PHARMACOLOGICAL EVALUATION; ANTIMICROBIAL ACTIVITY; TYROSINE KINASE; DESIGN; ANTITUMOR; AGENTS; ANTIMALARIAL; INHIBITORS;
D O I：
10.1007/s11094-020-02215-w
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Through a structure-based molecular hybridization strategy, a series of newN-acylhydrazone derivatives containing the benzothiazole and indole based moiety were designed, synthesized and screened forin vitroantiproliferative activity against Hep G2 cancer cell line. One compound (7a) exhibited excellent antiproliferative activity with IC(50)values of 0.78 mu M against Hep G2. In addition, C-5 substitutions of the indole ring of target compounds might be crucial for their cytotoxic activities. Additionally, the relative configuration of target compounds was confirmed as theEisomer. Further chemical manipulation of derivative 7a can make it possible to obtain new potential antitumor agents.
引用
收藏
页码：345 / 352
页数：8
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