Synthesis and biological activity of flavanone derivatives

被引：44

作者：

Shi, Lei ^{[1
]}

Feng, Xiu E. ^{[1
]}

Cui, Jing Rong ^{[2
]}

Fang, Lian Hua ^{[3
,4
]}

Du, Guan Hua ^{[3
,4
]}

Li, Qing Shan ^{[1
,2
]}

机构：

[1] Shanxi Med Univ, Sch Pharmaceut Sci, Taiyuan 030001, Peoples R China

[2] Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

[3] Chinese Acad Med Sci, Inst Mat Med, Beijing 100050, Peoples R China

[4] Peking Union Med Coll, Beijing 100050, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 18期

关键词：

Synthesis; Flavanone derivatives; Anti-tumor activity; PTK inhibitor; VSMC anti-vegetation activity; Cytoprotective activity; ATHEROSCLEROSIS;

D O I：

10.1016/j.bmcl.2010.07.090

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of new flavanone derivatives of farrerol was synthesized by a convenient method. The in vitro anti-tumor activity of these compounds was evaluated against human Bel-7402, HL-60, BGC-823 and KB cell lines, the protein tyrosine kinase (PTK) inhibitor activity was also tested. Their cytoprotective activity was tested using hydrogen peroxide (H2O2)-induced injury in human umbilical vein endothelial cells. Their in vitro anti-atherosclerosis activity was tested on vascular smooth muscle cells by the MTT method using tetrandrine as a positive contrast drug. The structures of all compounds synthesized were confirmed by H-1, C-13 NMR and ESI-MS. Most of the compounds exhibited good pharmacological activity and the preliminary structure-activity relationships were described. (c) 2010 Elsevier Ltd. All rights reserved.

引用

页码：5466 / 5468

页数：3

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