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

共 20 条

[1]

*CHIN AC MED SCI I, 1973, CHINESE HERBAL MED, V6, P31

[2] Naringin-induced p21WAF1-mediated G1-phase cell cycle arrest via activation of the Ras/Raf/ERK signaling pathway in vascular smooth muscle cells [J].

Lee, Eo-Jin ;

Moon, Gi-Seong ;

Choi, Won-Seok ;

Kim, Wun-Jae ;

Moon, Sung-Kwon .

FOOD AND CHEMICAL TOXICOLOGY, 2008, 46 (12) :3800-3807

[3]

EUN MH, 2008, BIOORGAN MED CHEM, V16, P6669

[4]

[韩光亮 Han Guangliang], 2005, [中国药理学通报, Chinese Pharmacological Bulletin], V21, P628

[5] FLAVONOIDS, A CLASS OF NATURAL-PRODUCTS OF HIGH PHARMACOLOGICAL POTENCY [J].

HAVSTEEN, B .

BIOCHEMICAL PHARMACOLOGY, 1983, 32 (07) :1141-1148

[6]

HWAJIN C, 2005, BIOORG MED CHEM LETT, V15, P3380

[7] Flavonoids in the species of Cyrtomium (Dryopteridaceae) and related genera [J].

Iwashina, T ;

Kitajima, J ;

Matsumoto, S .

BIOCHEMICAL SYSTEMATICS AND ECOLOGY, 2006, 34 (01) :14-24

[8]

JUNTEND KYT, 1988, Patent No. [292576, 0292576]

[9] Tyrosine kinase inhibitors in cancer therapy [J].

Madhusudan, S ;

Ganesan, TS .

CLINICAL BIOCHEMISTRY, 2004, 37 (07) :618-635

[10] Mechanisms of disease - Atherosclerosis - An inflammatory disease [J].

Ross, R .

NEW ENGLAND JOURNAL OF MEDICINE, 1999, 340 (02) :115-126

← 1 2 →