Design, synthesis and anti-tumor activity of novel 5-amino-2-(benzylthio) thia-zole-4-carboxamide derivatives / 中国药科大学学报
Journal of China Pharmaceutical University
;
(6): 16-22, 2017.
Article
in Chinese
| WPRIM
| ID: wpr-510553
ABSTRACT
A series of 5-amino-2-( benzylthio ) thiazole-4-carboxamide derivatives were designed and synthesized to discover novel compounds with anti-tumor activity. Compounds DDO-5401-DDO-5416 were synthesized using 2-amino-2-cyanoacetamide as the start material. The structures of the synthesized compounds were confirmed by IR, 1 H NMR and ESI-MS. The in vitro anti-tumor activities of the synthesized compounds were determined by MTT assay in HCT116 , HepG2 , A549 , MDA-MB-231 and MCF-7 cell lines. Target compounds showed good anti-tumor activity especially in A549 cell line. SAR study showed that electron donating groups were more favorable than electron absorption ones. Compound DDO-5413 exhibited noteworthy activity in MDA-MB-231 and MCF-7 cell lines with IC50 value lower than the positive reference dasatinib. It suggested that DDO-5413 might be the candidate for further investigation.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Journal of China Pharmaceutical University
Year:
2017
Type:
Article
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