Synthesis, anticancer and antioxidant activities of 2,4,5-trimethoxy chalcones and analogues from asaronaldehyde: Structure-activity relationship

被引：123

作者：

Shenvi, Suvarna ^{[1
]}

Kumar, Krishna ^{[1
]}

Hatti, Kaushik S. ^{[1
]}

Rijesh, K. ^{[1
]}

Diwakar, Latha ^{[1
]}

Reddy, G. Chandrasekara ^{[1
]}

机构：

[1] Vittal Mallya Sci Res Fdn, Bangalore 560076, Karnataka, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 62卷

关键词：

Chalcones; Flavones; Antioxidant; Anticancer; Flavonols; In-silico; BIOLOGICAL EVALUATION; CELL-CYCLE; METHOXYLATED CHALCONES; GROWTH-INHIBITION; DERIVATIVES; FLAVONOIDS; DESIGN;

D O I：

10.1016/j.ejmech.2013.01.018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2,4,5-Trimethoxy chalcones and analogues were synthesized from asaronaldehyde derived from beta-asarone. These novel compounds when tested against three human tumour cell lines (MCF-7, SW-982 and HeLa) using MTT assay, revealed that chalcones possessing electron donor groups in para position to carbonyl moiety of phenyl ring A, showed better inhibitory activity (2, 3, 4, 6, 7, 10, 17). When evaluated for antioxidant activities, compound 15 exhibited better free radical scavenging property in DPPH assay while compounds 2, 3, 5, 7, 9, 10, 11, 16, and 18 showed significant NO scavenging activity. All compounds exhibited very good phenyl hydrazine induced haemolysis of erythrocytes in phenylhydrazine assay. Structure activity relationship (SAR) study using in-silico analysis matched well with in-vitro tumour cell inhibitory activity. (C) 2013 Elsevier Masson SAS. All rights reserved.

引用

页码：435 / 442

页数：8

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