The homodimer approach to the design of a new long-acting depot prodrug of abiraterone

IF 1.8 4区化学 Q3 CHEMISTRY, MULTIDISCIPLINARY

Mendeleev Communications Pub Date : 2024-07-01 DOI:10.1016/j.mencom.2024.06.010

Evgeniya V. Nurieva , Oxana Yu. Kravtsova , Anna V. Sydoriuk , Elena V. Britikova , Vladimir V. Britikov , Nikolay A. Zefirov , Elena R. Milaeva , Olga N. Zefirova

引用次数: 0

Abstract

The synthesis of homodimeric bis-esters of abiraterone (an inhibitor of androgens synthesis used for treatment of prostate cancer) as a novel depot form of the drug intended for parenteral administration has been undertaken. The conjugate with succinic linker has been synthesized, while only mono-esters of malic and citric acid were obtained. The target ‘twin’ demonstrated excellent characteristics in preliminary biotests, proving the concept of long-lasting depot-prodrug.

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设计阿比特龙新型长效去势原药的同源二聚体方法

我们合成了阿比特龙（一种用于治疗前列腺癌的雄激素合成抑制剂）的同二聚体双酯，作为一种新型的肠外给药形式。我们合成了带有琥珀酸连接剂的共轭物，但只得到了苹果酸和柠檬酸的单酯。目标 "孪生 "在初步生物试验中表现出优异的特性，证明了长效去势药物的概念。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Mendeleev Communications 化学-化学综合

CiteScore

3.00

自引率

21.10%

发文量

226

审稿时长

4-8 weeks

期刊介绍： Mendeleev Communications is the journal of the Russian Academy of Sciences, launched jointly by the Academy of Sciences of the USSR and the Royal Society of Chemistry (United Kingdom) in 1991. Starting from 1st January 2007, Elsevier is the new publishing partner of Mendeleev Communications. Mendeleev Communications publishes short communications in chemistry. The journal primarily features papers from the Russian Federation and the other states of the former USSR. However, it also includes papers by authors from other parts of the world. Mendeleev Communications is not a translated journal, but instead is published directly in English. The International Editorial Board is composed of eminent scientists who provide advice on refereeing policy.