Developments of isoCombretastatin A-4 derivatives as highly cytotoxic agents.,European Journal of Medicinal Chemistry

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Developments of isoCombretastatin A-4 derivatives as highly cytotoxic agents.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-01-30 , DOI: 10.1016/j.ejmech.2020.112110
Abdallah Hamze ₁ , Mouad Alami ₁ , Olivier Provot ₁

Affiliation

Combretastatin A-4 (CA-4) is a natural anti-cancer agent isolated in 1989 from the African willow tree, Combretum caffrum. Due to its chemical simplicity, this (Z)-stilbene has been the subject of many structural modifications mainly to improve its chemical and metabolic stability. Beside a large number of synthetic analogues, isoCombretastatin A-4 (isoCA-4), has proved to be a solution of choice since this non-natural isomer of CA-4 is stable, easier to synthesize and has equivalent antitumor properties as CA-4. In this review, we will present the structure-activity relationships (SARs) around isoCA-4 since its discovery in 2007. In a first part, we will describe some alternatives to replace the phenol B-ring of isoCA-4, then we will focus on the variations made on the 1,1-ethylene double bond and then, we will evocate very recent exiting results concerning the possible replacements of the 3,4,5-trimethoxyphenyl A-ring of isoCA-4 by suitable heterocycles.

中文翻译：

isoCombretastatin A-4衍生物作为高度细胞毒性药物的开发。

Combretastatin A-4（CA-4）是一种天然抗癌剂，于1989年从非洲柳树Combretum caffrum中分离出来。由于其化学简单性，这种（Z）-二苯乙烯已成为许多结构修饰的主题，主要是为了改善其化学和代谢稳定性。除了大量合成类似物外，isoCombretastatin A-4（isoCA-4）已被证明是一种选择的解决方案，因为CA-4的这种非天然异构体稳定，易于合成并且具有与CA-等效的抗肿瘤特性4。在本综述中，我们将介绍自2007年发现以来isoCA-4周围的结构-活性关系（SAR）。在第一部分中，我们将描述一些替代isoCA-4的酚B环的替代方法，然后我们将介绍专注于1,1-乙烯双键的变化，然后，

更新日期：2020-01-31

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