Design, synthesis and biological evaluation of novel stilbene-based antitumor agents

被引：26

作者：

Simoni, Daniele ^{[1
]}

Invidiata, Francesco Paolo ^{[2
]}

Eleopra, Marco ^{[1
]}

Marchetti, Paolo ^{[1
]}

Rondanin, Riccardo ^{[1
]}

Baruchello, Riccardo ^{[1
]}

Grisolia, Giuseppina ^{[1
]}

Tripathi, Ashutosh ^{[3
,4
]}

Kellogg, Glen E. ^{[3
,4
]}

Durrant, David ^{[5
]}

Lee, Ray M. ^{[5
]}

机构：

[1] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy

[2] Univ Palermo, Dipartimento Farmacochim Tossicol & Biol, I-90133 Palermo, Italy

[3] Virginia Commonwealth Univ, Dept Med Chem, Richmond, VA 23298 USA

[4] Virginia Commonwealth Univ, Inst Struct Biol & Drug Discovery, Richmond, VA 23298 USA

[5] Virginia Commonwealth Univ, Massey Canc Ctr, Richmond, VA 23298 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 02期

关键词：

Antitumor agents; Stilbenes; Prodrugs; RESVERATROL; INHIBITORS; ANALOGS; CELLS;

D O I：

10.1016/j.bmc.2008.12.002

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of novel stilbene derivatives has been synthesized and studied with the main goal to investigate SAR of the amino compound 1a, as well as to improve its water solubility, a potentially negative aspect of the molecule that could be a serious obstacle for a pre-clinical development. We have obtained derivatives with good cytotoxic activity, in particular, the derivatives 5c and 6b could represent two novel leads for further investigation. Compound 8b, a morpholino-carbamate derivative, prodrug of 1a, has a very good solubility in water, and is active in suppressing growth of tumor cells at a concentration of 5000 nM, which is a concentration 100 times higher than the parent stilbene 1a. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：512 / 522

页数：11

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