间苯二酚类Hsp90抑制剂的重新筛选和体外初步评价

IF 0.8 4区化学 Q4 CHEMISTRY, MULTIDISCIPLINARY

South African Journal of Chemistry-Suid-Afrikaanse Tydskrif Vir Chemie Pub Date : 2023-01-01 DOI:10.17159/0379-4350/2023/v77a04

T. Umumararungu, M. Isaacs, H. Hoppe, E. Goosen, S. Khanye

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引用次数: 0

摘要

本研究探索了一系列间苯二酚衍生物，这些衍生物最初被鉴定为热休克蛋白90抑制剂，具有抗原生动物寄生虫的活性。结果表明，部分化合物对氯喹敏感型恶性疟原虫(3D7)和布鲁氏锥虫(10 μM以下)有活性，对25 μM的人宫颈腺癌(HeLa)细胞无明显细胞毒作用。

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Re-screening and preliminary in vitro evaluation of resorcinol based Hsp90 inhibitors for potential protocidal activity

This study explored a series of resorcinol derivatives originally identified as heat shock protein 90 inhibitors for activity against protozoan parasites. The repurposing of this series revealed that some of these compounds are active against chloroquine-sensitive Plasmodium falciparum (3D7) and Trypanosoma brucei brucei strains with IC50 values below 10 μM without obvious cytotoxic effects against human cervix adenocarcinoma (HeLa) cells at 25 μM.

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来源期刊

South African Journal of Chemistry-Suid-Afrikaanse Tydskrif Vir Chemie 化学-化学综合

CiteScore

3.10

自引率

0.00%

发文量

审稿时长

>12 weeks

期刊介绍： Original work in all branches of chemistry is published in the South African Journal of Chemistry. Contributions in English may take the form of papers, short communications, or critical reviews.