Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives

A 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-2...

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Bibliographic Details
Published in:Chemical research in Chinese universities 2013-02, Vol.29 (1), p.62-66
Main Authors: Zhai, Xin, He, Ying, Yang, Zhen, Gong, Ping
Format: Article
Language:English
Subjects:
Analytical Chemistry
Chemistry
Chemistry and Materials Science
Chemistry/Food Science
IC50
Inorganic Chemistry
Organic Chemistry
Physical Chemistry
上皮细胞
合成
增殖活性
细胞毒性
肺癌细胞
肿瘤细胞株
衍生物
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Summary:A 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）thiazolyldiphenyltetrazoliumromide（MTT） assay. Six compounds（Tb--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.
ISSN:1005-9040
2210-3171
DOI:10.1007/s40242-013-2136-5