Synthesis and activity of β-carboline antimalarials targeting the Plasmodium falciparum heat shock 90 protein

被引：10

作者：

Viswanathan, Neil K. ^{[1
]}

Chirgwin, Michael E. ^{[2
]}

Gibbs, Julia ^{[1
]}

Kalaj, Brianna N. ^{[3
]}

Durham, Sierra ^{[4
]}

Tran, Jennifer ^{[1
]}

Gomez, Maximillian ^{[1
]}

Lazaro, Horacio ^{[5
]}

Chen, Ming ^{[5
]}

Mansfield, Christopher R. ^{[6
]}

Derbyshire, Emily R. ^{[2
]}

Eagon, Scott ^{[1
]}

机构：

[1] Calif Polytech State Univ San Luis Obispo, Dept Chem & Biochem, San Luis Obispo, CA 93407 USA

[2] Duke Univ, Dept Chem, Durham, NC 27708 USA

[3] Univ Calif San Diego, Dept Chem & Biochem, San Diego, La Jolla, CA 92093 USA

[4] Univ Calif Davis, Dept Food Sci & Technol, Davis, CA 95616 USA

[5] Promega Biosci, 277 Granada Dr, San Luis Obispo, CA 93401 USA

[6] Duke Sch Med, Dept Mol Genet & Microbiol, Durham, NC 27708 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2023年 / 92卷

关键词：

Malaria; Plasmodium falciparum; Beta-carbolines; Heat shock 90 protein; HSP90;

D O I：

10.1016/j.bmcl.2023.129410

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A collection of & beta;-carbolines based on the natural product harmine, a compound known to target the heat shock 90 protein of Plasmodium falciparum, was synthesized and tested for antimalarial activity and potential toxicity. Several of these novel compounds display promising bioactivity, providing a new potential therapeutic with a mode of action that differs versus any currently available clinical treatment.

引用

页数：4

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