Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents

IMR OpenIR

	Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents
其他题名	Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents
	Ma Junjie 1; Hu Gang 1; Xie Lijun 2; Chen Lei 1; Xu Boxuan 1; Gong Ping 1
	2015
发表期刊	CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN	1005-9040
卷号	31 期号:6 页码:958-963
摘要	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.
其他摘要	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.
关键词	POTENT INHIBITORS ONCRASIN-1 DISCOVERY Benzothiazole Semicarbazone Antitumor activity
收录类别	CSCD
语种	英语
资助项目	[Program for Liaoning Excellent Talents in University, China] ; [National Natural Science Foundation of China]
CSCD记录号	CSCD:5586213
引用统计	被引频次：5[CSCD] [CSCD记录]
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/144342
专题	中国科学院金属研究所
作者单位	1.中国科学院金属研究所 2.Fujian Institute Microbiol, Fuzhou 350007, Peoples R China
推荐引用方式 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.