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冬凌草甲素及其衍生物用于抗癌药物设计。

Lycorine and its derivatives for anticancer drug design.

机构信息

Laboratoire de Chimie Analytique,Toxicologie et Chimie Physique Appliquée, Institut de Pharmacie, Université Libre de Bruxelles, Brussels, Belgium.

出版信息

Mini Rev Med Chem. 2010 Jan;10(1):41-50. doi: 10.2174/138955710791112604.

Abstract

Amaryllidaceae alkaloids are extensively studied for their biological activities in several pharmaceutical areas, including, for example, Alzheimer's disease for which galanthamine has already reached the market. Among this chemical family, lycorine displays very promising anti-tumor properties. This review first focuses on the chemical diversity of natural and synthetic analogues of lycorine and their metabolites, and then on mechanisms of action and biological targets through which lycorine and its derivatives display their anti-tumor activity. Our analysis of the structure-activity relationships of this family of compounds highlights the existence of various potential leads for the development of novel anticancer agents.

摘要

石蒜科生物碱因其在多个制药领域的生物活性而被广泛研究,例如,加兰他敏已经上市用于治疗阿尔茨海默病。在这个化学家族中,石蒜碱显示出非常有前途的抗肿瘤特性。这篇综述首先集中讨论了石蒜碱的天然和合成类似物及其代谢物的化学多样性,然后讨论了石蒜碱及其衍生物发挥抗肿瘤活性的作用机制和生物靶点。我们对这类化合物的构效关系的分析强调了存在各种潜在的先导化合物,可用于开发新型抗癌药物。

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