发现具有抗癌潜力的肉桂酸衍生物的方法。

IF 6 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Expert Opinion on Drug Discovery Pub Date : 2024-10-01 Epub Date: 2024-08-06 DOI:10.1080/17460441.2024.2387122
Ioannis Fotopoulos, Dimitra Hadjipavlou-Litina
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引用次数: 0

摘要

简介:肉桂酸是设计具有潜在抗癌潜力的生物活性化合物的重要支架,可采用不同的合成方法和程序。由于生产强效抗癌剂的需要,肉桂酸分子可以为设计新的、更有活性的抗癌剂做出重大贡献:在这篇综述中,作者综述了发现具有抗癌潜力的肉桂酸衍生物的合成方法。作者给出、描述并讨论了分子模拟、杂交和化学衍生的结果,以及体外生物实验和结构活性关系。有关作用机制的信息来自原始文献资料:作者建议:(i) 需要考虑生物学-药理学的多个领域:选择性、体内研究、毒性和药物相似性、动物和人体的作用机制、针对各种癌症类型开发更有效的检测方法;(ii) 杂交技术在发现和生产具有更高活性和更大选择性的化合物方面发挥了平衡作用;(iii) 重新定位提供了新的抗癌肉桂药剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Approaches for the discovery of cinnamic acid derivatives with anticancer potential.

Introduction: Cinnamic acid is a privileged scaffold for the design of biologically active compounds with putative anticancer potential, following different synthetic methodologies and procedures. Since there is a need for the production of potent anticancer, cinnamate moiety can significantly contribute in the design of new and more active anticancer agents.

Areas covered: In this review, the authors provide a review on the synthetic approaches for the discovery of cinnamic acid derivatives with anticancer potential. Results from molecular simulations, hybridization, and chemical derivatization along with biological experiments in vitro and structural activity relationships are given, described, and discussed by the authors. Information for the mechanism of action is taken from original literature sources.

Expert opinion: The authors suggest that (i) numerous areas of biology-pharmacology need to be considered: selectivity, in vivo studies, toxicity and drug-likeness, the mechanism of action in animals and humans, development of more efficient assays for various cancer types; (ii) hybridization techniques outbalance in the discovery and production of compounds with higher activity and greater selectivity; (iii) repositioning offers new anticancer cinnamic agents.

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来源期刊
CiteScore
10.20
自引率
1.60%
发文量
78
审稿时长
6-12 weeks
期刊介绍: Expert Opinion on Drug Discovery (ISSN 1746-0441 [print], 1746-045X [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on novel technologies involved in the drug discovery process, leading to new leads and reduced attrition rates. Each article is structured to incorporate the author’s own expert opinion on the scope for future development. The Editors welcome: Reviews covering chemoinformatics; bioinformatics; assay development; novel screening technologies; in vitro/in vivo models; structure-based drug design; systems biology Drug Case Histories examining the steps involved in the preclinical and clinical development of a particular drug The audience consists of scientists and managers in the healthcare and pharmaceutical industry, academic pharmaceutical scientists and other closely related professionals looking to enhance the success of their drug candidates through optimisation at the preclinical level.
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