Design and synthesis of novel 2'-hydroxy group substituted 2-pyridone derivatives as anticancer agents.

Abstract

We have synthesized a series of novel 2-pyridone derivatives with 1,2,3-triazole and evaluated their anti-tumor activities in vitro. The bioassays showed that the majority of the resultant compounds exerted inhibitory effects on six human cancer cell lines to various extents. In particular, compound 10k showed the best anti-tumor activities (IC50 values of A549, HeLa and SW480 cancer cell lines were 0.86 ± 0.17 μM, 0.54 ± 0.23 μM and 0.21 ± 0.13 μM, respectively).

• Authors: Zhiliang Lv, Yikai Zhang, Mingfeng Zhang, Huan Chen, Zhenliang Sun, Dongping Geng, Chunjuan Niu, Ke Li
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 67 Pg. 447-53 (Sep 2013) ISSN: 1768-3254 [Electronic] France
• PMID: 23920246 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2013 Elsevier Masson SAS. All rights reserved.

Chemical References

• Antineoplastic Agents
• Pyridones
• 2-hydroxypyridine

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Dose-Response Relationship, Drug
• Drug Design
• Drug Screening Assays, Antitumor
• HeLa Cells
• Humans
• Molecular Structure
• Pyridones (chemical synthesis, chemistry, pharmacology)
• Structure-Activity Relationship