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Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents
Alternative TitleDesign, 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 PublicationCHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN1005-9040
Volume31Issue:6Pages:958-963
AbstractA 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 AbstractA 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.
KeywordPOTENT INHIBITORS ONCRASIN-1 DISCOVERY Benzothiazole Semicarbazone Antitumor activity
Indexed ByCSCD
Language英语
Funding Project[Program for Liaoning Excellent Talents in University, China] ; [National Natural Science Foundation of China]
CSCD IDCSCD:5586213
Citation statistics
Cited Times:4[CSCD]   [CSCD Record]
Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/144339
Collection中国科学院金属研究所
Affiliation1.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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