利用温和的环化反应高效筛选基于芳基氮吡唑的可光开关 CENP-E 抑制剂的化学平台。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2024-07-17 DOI:10.1016/j.bmcl.2024.129892

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引用次数: 0

摘要

在温和的条件下，利用 1,3-二酮中间体与各种肼的定量环化反应，通过化学平台发现了一组针对有丝分裂运动蛋白 CENP-E 的芳基吡唑抑制剂。通过这一高效平台，成功地阐明了光开关 CENP-E 抑制剂中吡唑光开关的结构-活性关系，不仅在体外，而且在细胞中也是如此。

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A chemical platform for the efficient screening of arylazopyrazole-based photoswitchable CENP-E inhibitors using mild cyclization reactions

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A chemical platform for the efficient screening of arylazopyrazole-based photoswitchable CENP-E inhibitors using mild cyclization reactions

A set of arylazopyrazole-based inhibitors targeting the mitotic motor protein CENP-E was discovered through the chemical platform using the quantitative cyclization of 1,3-diketone intermediate with various hydrazines under mild conditions. Through this efficient platform, the structure–activity relationship pertaining to the pyrazole photoswitch in photoswitchable CENP-E inhibitors not only in vitro but also in cells was successfully clarified.

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.