Synthesis of a novel prodrug of 3-(4′-geranyloxy-3′-methoxyphenyl)-2-trans-propenoic acid for colon delivery

被引：23

作者：

Curini, M ^{[1
]}

Epifano, F ^{[1
]}

Genovese, S ^{[1
]}

机构：

[1] Sez Chim Organ, Dipartimento Chim & Tecnol Farm, I-06123 Perugia, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 22期

关键词：

cinnamic acids; colon delivery; colon cancer; ferulic acid derivatives; prodrug;

D O I：

10.1016/j.bmcl.2005.07.088

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel high-yielding and environment-friendly synthesis of the anticancer compound 3-(4'-geranyloxy-3'-methoxyphenyl)-2-trans-propenoic acid is described. This compound was conjugated to H2N-Ala-Pro dipeptide to give a prodrug to be activated by intestinal ACE and to be used in the treatment of different forms of colon cancer. Data on the chemical and enzymatic stability of this novel prodrug are reported. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：5049 / 5052

页数：4

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