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Diarylpentanoids with antitumor activity: A critical review of structure-activity relationship studies
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2020-02-27 , DOI: 10.1016/j.ejmech.2020.112177
Joana Moreira , Lucilia Saraiva , Madalena M. Pinto , Honorina Cidade

Diarypentanoids are commonly considered as monocarbonyl analogues of curcumin. Since the discovery of this compound in 1962, twenty one diarylpentanoids have been isolated and almost 600 synthetic analogues with antitumor activity have been synthesized. This review reports the exploitation of diarylpentanoids to develop curcumin analogues with improved antitumor activity over the last two decades. The mechanism of action and structure-activity relationship (SAR) studies are also highlighted. More importantly, structural features for the antitumor activity that may guide the design of new and more effective diarylpentanoids are also proposed.



中文翻译:

具有抗肿瘤活性的二芳基戊烷类化合物:结构-活性关系研究的重要综述

二芳基戊二酸酯通常被认为是姜黄素的单羰基类似物。自1962年发现该化合物以来,已分离出21种二芳基戊烷,并合成了近600种具有抗肿瘤活性的合成类似物。这篇综述报道了在过去的二十年中,利用二芳基戊烷类化合物开发了姜黄素类似物,具有改善的抗肿瘤活性。还强调了作用机理和结构-活性关系(SAR)研究。更重要的是,还提出了可指导新的和更有效的二芳基戊烷类药物设计的抗肿瘤活性的结构特征。

更新日期:2020-02-27
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