Synthesis of fusidane triterpenoid Mannich bases as potential antibacterial and antitumor agents

被引：2

作者：

Salimova, Elena V. ^{[1
]}

Parfenova, Lyudmila V. ^{[1
]}

Ishmetova, Diana V. ^{[2
]}

Zainullina, Liana F. ^{[2
]}

Vakhitova, Yulia V. ^{[2
]}

机构：

[1] Russian Acad Sci, Inst Petrochem & Catalysis, Ufa Fed Res Ctr, Ufa, Russia

[2] Russian Acad Sci, Inst Biochem & Genet, Ufa Fed Res Ctr, Ufa, Russia

来源：

NATURAL PRODUCT RESEARCH | 2023年 / 37卷 / 23期

基金：

英国惠康基金;

关键词：

Fusidane triterpenoids; Mannich bases; propargyl group; anticancer activity; antibacterial activity; fungicidal activity; ANTIMALARIAL ACTIVITY; BIOLOGICAL-ACTIVITY; MOLECULAR DOCKING; AMIDE DERIVATIVES; NATURAL-PRODUCTS; BINDING-SITE; ACID; DISCOVERY;

D O I：

10.1080/14786419.2022.2163483

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Mannich bases (8 examples) were synthesized via aminomethylation of fusidane propargyl esters. In vitro antimicrobial screening against key ESKAPE pathogens showed that the fusidic acid based Mannich products exhibit a high antimicrobial effect against Gram-positive bacteria Staphylococcus aureus and the fungus Cryptococcus neoformans. Moreover, the cytotoxic effect of fusidic acid and its analogs, which showed high antibacterial activity, was determined by MTT assay on cancer HepG2, HCT-116, SH-SY5Y, MCF-7, A549 and conditionally normal cells HEK293. A remarkable cytotoxic activity of fusidic acid propargyl ester and its aminomethylene derivatives against cancer and nontumoral HEK293 cells with IC50 values within 4.2-25 mu M was found.

引用

页码：3956 / 3963

页数：8

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