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Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives
Alternative TitleSyntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives
Zhai Xin; He Ying; Yang Zhen; Gong Ping
2013
Source PublicationCHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN1005-9040
Volume29Issue:1Pages:62-66
AbstractA series of novel N-methylpicolinamide-moiety containing diarylthiosemicarbazide derivatives was prepared and evaluated for their in vitro antiproliferative activity against three cancer cell lines(human alveolar epithelial cell A549, human lung cancer cell 11460 and human colorectal cancer cell HT-29) by 3-(4,5-dimethyl)thiazolyl-diphenyltetrazoliumromide(MTT) assay. Six compounds(7b-7g) with halogen substituents exhibited preferable cytotoxicity against one or more cell lines in a low micromolar range. Especially, the most promising compound 7g exhibited remarkable antiproliferative activity with the IC50 values of 2.2, 1.8 and 5.2 mu mol/L against A549, 11460 and HT-29 cell lines respectively, which is comparable to sorafenib.
Other AbstractA series of novel N-methylpicolinamide-moiety containing diarylthiosemicarbazide derivatives was prepared and evaluated for their in vitro antiproliferative activity against three cancer cell lines(human alveolar epithelial cell A549,human lung cancer cell H460 and human colorectal cancer cell HT-29) by 3-(4,5-dimethyl)thiazolyl- diphenyltetrazoliumromide(MTT) assay. Six compounds(7b―7g) with halogen substituents exhibited preferable cytotoxicity against one or more cell lines in a low micromolar range. Especially,the most promising compound 7g exhibited remarkable antiproliferative activity with the IC50 values of 2.2,1.8 and 5.2 μmol/L against A549,H460 and HT-29 cell lines respectively,which is comparable to sorafenib.
KeywordKINASE INHIBITORS ANTITUMOR AGENTS DESIGN BENZIMIDAZOLES CYTOTOXICITY Thiosemicarbazide N-methylpicolinamide Antiproliferative activity
Indexed ByCSCD
Language英语
Funding Project[National Natural Science Foundation of China] ; [Science & Technology Project of Liaoning Province, China]
CSCD IDCSCD:4756394
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Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/146988
Collection中国科学院金属研究所
Affiliation中国科学院金属研究所
Recommended Citation
GB/T 7714
Zhai Xin,He Ying,Yang Zhen,et al. Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives[J]. CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,2013,29(1):62-66.
APA Zhai Xin,He Ying,Yang Zhen,&Gong Ping.(2013).Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives.CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,29(1),62-66.
MLA Zhai Xin,et al."Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives".CHEMICAL RESEARCH IN CHINESE UNIVERSITIES 29.1(2013):62-66.
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