Synthesis, cytotoxicity and computational study of novel protoberberine derivatives

A novel and efficient synthetic route has been developed for the preparation of protoberberine derivatives. The methodology designed to control, primarily, substitution patterns on the terminal rings, was used to access a small array of these compounds. Initial biological profiling suggested antican...

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Bibliographic Details
Published inJournal of the Serbian Chemical Society Vol. 81; no. 2; pp. 103 - 123
Main Authors Simic, Milena, Damjanovic, Ana, Kalinic, Marko, Tasic, Gordana, Eric, Slavica, Antic-Stankovic, Jelena, Savic, Vladimir
Format Journal Article
LanguageEnglish
Published Belgrade Journal of the Serbian Chemical Society 01.01.2016
Serbian Chemical Society
Subjects
Access control
cytotoxic properties
Derivatives
Fishing
Lead compounds
privileged structure
protoberberine
synthesis
target fishing
Target recognition
Toxicity
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Summary:A novel and efficient synthetic route has been developed for the preparation of protoberberine derivatives. The methodology designed to control, primarily, substitution patterns on the terminal rings, was used to access a small array of these compounds. Initial biological profiling suggested anticancer potential of synthesised derivatives while structure-based target fishing has identified their potential targets and has established rational bases for further structural modifications. Although the activities need further improvement, our study demonstrated that the described approach may be useful in the discovery of the novel lead compounds.
ISSN:0352-5139
1820-7421
DOI:10.2298/JSC150525090S