In vitro biological evaluation of novel 7-O-dialkylaminoalkyl cytotoxic pectolinarigenin derivatives against a panel of human cancer cell lines

被引：38
|
作者：
Bonesi, Marco [1 ]
Tundis, Rosa [1 ]
Deguin, Brigitte [2 ]
Loizzo, Monica R. [1 ]
Menichini, Federica [3 ]
Tillequin, Francois [2 ]
Menichini, Francesco [1 ]
机构：
[1] Univ Calabria, Fac Pharm & Nutr & Hlth Sci, Dept Pharmaceut Sci, I-87036 Arcavacata Di Rende, CS, Italy
[2] Univ Paris 05, Fac Sci Pharmaceut & Biol, CNRS, Lab Pharmacognosie,UMR 8638, F-75006 Paris, France
[3] Kings Coll London, Dept Pharm, Pharmacognosy Res Labs, London SE1 9NN, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 20期
关键词：
cytotoxic activity; pectolinarigenin; dialkylaminoalkyl side chain;
D O I：
10.1016/j.bmcl.2008.09.037
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The effect of novel pectolinarigenin derivatives bearing a dialkylaminoalkyl substituent at O-7 on cell proliferation was evaluated in vitro in a panel of seven human cancer cell lines including renal adenocarcinoma ACHN, amelanotic melanoma C32, colorectal adenocarcinoma Caco-2, lung large cell carcinoma COR-L23, malignant melanoma A375, lung carcinoma A549 and hepatocellular carcinoma Huh-7D12 cell lines. Pectolinarigenin (2), obtained by hydrolysis of rutinose unit of the pectolinarin (1) isolated from Linaria reflexa, exhibited cytotoxic activity against Caco-2, A549 and A375 cell lines with IC50 values of 5.3-8.2 mu M. The most active pectolinarigenin derivative was 3 characterized by a dimethylamino-propoxy group in O-7 with IC50 values of 7.2 and 7.4 mu M against COR-L23 and A549 cell lines, respectively. A structure-activity relationship analysis of synthesized compounds was performed. None of the tested compounds affected the proliferation of skin. broblasts 142BR suggesting a selective activity against tumor cells. (C) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5431 / 5434
页数：4
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