Synthesis of 4-Hydroxy-2-pyridinone Derivatives and Evaluation of Their Antioxidant/Anticancer Activities

被引：17

作者：

Hamama, Wafaa S. ^{[1
]}

Ghaith, Eslam A. ^{[1
]}

Ibrahim, Mona E. ^{[1
]}

Sawamura, Masaya ^{[2
]}

Zoorob, Hanafi H. ^{[1
]}

机构：

[1] Mansoura Univ, Fac Sci, Dept Chem, Mansoura 35516, Egypt

[2] Hokkaido Univ, Inst Chem React Design & Discovery WPI ICReDD, Sapporo, Hokkaido 0010021, Japan

来源：

CHEMISTRYSELECT | 2021年 / 6卷 / 07期

关键词：

Antioxidants; Cytotoxic Activity; Dehydroacetic acid; Mechanisms; Molecular Modeling; Pyridinone; Reactions;

D O I：

10.1002/slct.202004682

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A simple approach was applied for the regioselective synthesis of various pyridine-2-one derivatives or annulated pyridine as novel heterocyclic systems from the reaction of dehydroacetic acid (DHA) with mono- or bidentate nucleophile as with benzylamine and/or phenylenediamines in dichloromethane followed by transformation with different halo-compounds in refluxing 1,4-dioxane has been achieved in moderate to excellent yields (48-93 %). In addition, DFT studies of the key synthesized compounds were carried out for confirmed proposed mechanisms. The newly synthesized compounds were screened for their in-vitro inhibition activities against mammary gland breast cancer (MCF-7) and human prostate cancer (PC-3) using the MTT colorimetric method. Also, the target synthesized compounds were evaluated as antioxidant agents.

引用

页码：1430 / 1439

页数：10

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