Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 14, Pages 3263-3270Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.05.059
Keywords
1,3-Thiazole; Carboxamide; Hydrazide-hydrazone; Antitumor activity; Apoptosis
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Funding
- National Basic Research Program of China [2010CB126100]
- National Natural Science Foundation of China [21172090, 21472062]
- Natural Science Key Foundation of Hubei Province [2014CFA111]
- Excellent Doctorial Dissertation Cultivation Grant From Central China Normal University
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A series of novel 2,4,5-trisubstituted 1,3-thiazole derivatives containing hydrazide-hydrazine, and carboxamide moiety including 46 compounds T were synthesized, and evaluated for their antitumor activity in vitro against a panel of five human cancer cell lines. Eighteen title compounds T displayed higher inhibitory activity than that of 5-Fu against MCF-7, HepG2, BGC-823, Hela, and A549 cell lines. Especially, T1, T26 and T38 exhibit best cytotoxic activity with IC50 values of 2.21 mu g/mL, 1.67 mu g/mL and 1.11 mu g/mL, against MCF-7, BCG-823, and HepG2 cell lines, respectively. These results suggested that the combination of 1,3-thiazole, hydrazide-hydrazone, and carboxamide moiety was much favorable to cytotoxicity activity. Furthermore, the flow cytometry analysis revealed that compounds T1 and T38 could induce apoptosis in HepG2 cells, and it was confirmed T38 led the induction of cell apoptosis by S cell-cycle arrest. (C) 2016 Elsevier Ltd. All rights reserved.
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