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WANG Lu, YOU Qidong, JIANG Zhengyu. Design, synthesis and anti-tumor activity of novel 5-amino-2-(benzylthio)thiazole-4-carboxamide derivatives[J]. Journal of China Pharmaceutical University, 2017, 48(1): 16-22. DOI: 10.11665/j.issn.1000-5048.20170103
Citation: WANG Lu, YOU Qidong, JIANG Zhengyu. Design, synthesis and anti-tumor activity of novel 5-amino-2-(benzylthio)thiazole-4-carboxamide derivatives[J]. Journal of China Pharmaceutical University, 2017, 48(1): 16-22. DOI: 10.11665/j.issn.1000-5048.20170103
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Design, synthesis and anti-tumor activity of novel 5-amino-2-(benzylthio)thiazole-4-carboxamide derivatives

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  • 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, 1H 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.
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