柔红霉素与3,4-亚甲二氧基苯甲醛共轭物的合成及其抗肿瘤活性

Synthesis and antitumor activity of daunorubicin conjugates with of 3,4-methylendioxybenzaldehyde.

作者信息

Moiseeva Aleksandra A, Artyushin Oleg I, Anikina Lada V, Brel Valery K

机构信息

A. N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, ul. Vavilova 28, Moscow 119991, Russia.

Institute of Physiologically Active Compounds, Russian Academy of Sciences, 1 Severny pr., Chernogolovka 142432, Russia.

出版信息

Bioorg Med Chem Lett. 2019 Oct 1;29(19):126617. doi: 10.1016/j.bmcl.2019.08.021. Epub 2019 Aug 12.

DOI:10.1016/j.bmcl.2019.08.021

PMID:31431363

Abstract

The design of hybrid (chimeric) molecules containing two different pharmacophores connected via a spacer (linker) is a promising approach to the functionalization of natural compounds and potentially of drug molecules. These are important examples for the use of this approach with anthracycline antibiotics. The use of this methodology may help to eliminate some of the drawbacks of anthracycline drugs, e.g., high cardiotoxicity and MDR development.

摘要

设计通过间隔基（连接子）连接两种不同药效基团的杂合（嵌合）分子，是使天然化合物以及潜在地使药物分子功能化的一种有前景的方法。这些是将此方法用于蒽环类抗生素的重要实例。使用这种方法可能有助于消除蒽环类药物的一些缺点，例如高心脏毒性和多药耐药性的产生。