Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents | |
Alternative Title | Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents |
Ma Junjie1; Hu Gang1; Xie Lijun2; Chen Lei1; Xu Boxuan1; Gong Ping1 | |
2015 | |
Source Publication | CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
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ISSN | 1005-9040 |
Volume | 31Issue:6Pages:958-963 |
Abstract | A series of novel benzothiazole derivatives bearing semicarbazone as a linker was designed and synthesized, and their in vitro antitumor activities were evaluated against four cancer cell lines(HT29, 11460, A549 and MDA-MB-231). Most of them showed moderate to excellent activity against all the tested cell lines. Among them, compounds 12a-12i with fluoro-substituted benzyl-1H-indole moiety displayed more potent activity than those with phenyl moiety. The most promising compound 12d exhibited excellent antitumor activity with IC50 values of 0.015, 0.28, 1.53 and 0.68 mu mol/L against the four tested cell lines respectively. |
Other Abstract | A series of novel benzothiazole derivatives bearing semicarbazone as a linker was designed and synthesized, and their in vitro antitumor activities were evaluated against four cancer cell lines(HT29, H460, A549 and MDA-MB-231). Most of them showed moderate to excellent activity against all the tested cell lines. Among them, compounds 12a―12i with fluoro-substituted benzyl-1H-indole moiety displayed more potent activity than those with phenyl moiety. The most promising compound 12d exhibited excellent antitumor activity with IC_(50) values of 0.015, 0.28, 1.53 and 0.68 μmol/L against the four tested cell lines respectively. |
Keyword | POTENT INHIBITORS ONCRASIN-1 DISCOVERY Benzothiazole Semicarbazone Antitumor activity |
Indexed By | CSCD |
Language | 英语 |
Funding Project | [Program for Liaoning Excellent Talents in University, China] ; [National Natural Science Foundation of China] |
CSCD ID | CSCD:5586213 |
Citation statistics |
Cited Times:4[CSCD]
[CSCD Record]
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Document Type | 期刊论文 |
Identifier | http://ir.imr.ac.cn/handle/321006/144342 |
Collection | 中国科学院金属研究所 |
Affiliation | 1.中国科学院金属研究所 2.Fujian Institute Microbiol, Fuzhou 350007, Peoples R China |
Recommended Citation GB/T 7714 | Ma Junjie,Hu Gang,Xie Lijun,et al. Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents[J]. CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,2015,31(6):958-963. |
APA | Ma Junjie,Hu Gang,Xie Lijun,Chen Lei,Xu Boxuan,&Gong Ping.(2015).Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents.CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,31(6),958-963. |
MLA | Ma Junjie,et al."Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents".CHEMICAL RESEARCH IN CHINESE UNIVERSITIES 31.6(2015):958-963. |
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