Design, synthesis and anti-tumor activity of novel 5-amino-2-(benzylthio) thia-zole-4-carboxamide derivatives
10.11665/j.issn.1000-5048.20170103
- VernacularTitle:新型5-氨基-2-（苄基硫代）噻唑-4-甲酰胺类化合物的设计、合成及抗肿瘤活性
- Author:
Lu WANG
;
Qidong YOU
;
Zhengyu JIANG
- Keywords:
5-amino-2-( benzylthio) thiazole-4-carboxamide derivatives;
synthesis;
anti-tumor activity
- From:
Journal of China Pharmaceutical University
2017;48(1):16-22
- CountryChina
- Language:Chinese
-
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.
