Synthesis, analysis and biological evaluation of novel indolquinonecryptolepine analogues as potential anti-tumour agents.

Le Gresley, A, Gudivaka, V, Carrington, S, Sinclair, A and Brown, J E (2016) Synthesis, analysis and biological evaluation of novel indolquinonecryptolepine analogues as potential anti-tumour agents. Organic & Biomolecular Chemistry, 14, pp. 3069-3079. ISSN (print) 1477-0520

Full text available as:
[img]
Preview
Text
Le Gresley_34556_VoR.pdf - Published Version
Available under License Creative Commons Attribution.

Download (1MB) | Preview

Abstract

A small library of cryptolepine analogues were synthesised incorporating halogens and/or nitrogen containing side chains to optimise their interaction with the sugar-phosphate backbone of DNA to give improved binding, interfering with topoisomerase II hence enhancing cytotoxicity. Cell viability, DNA binding and Topoisomerase II inhibition is discussed for these compounds. Fluorescence microscopy was used to investigate the uptake of the synthesised cryptolepines into the nucleus. We report the synthesis and anti-cancer biological evaluation of nine novel cryptolepine analogues, which have greater cytotoxicity than the parent compound and are important lead compounds in the development of novel potent and selective indoloquinone anti-neoplastic agents.

Item Type: Article
Research Area: Chemistry
Faculty, School or Research Centre: Faculty of Science, Engineering and Computing
Faculty of Science, Engineering and Computing > School of Pharmacy and Chemistry
Related URLs:
Depositing User: Automatic Import Agent
Date Deposited: 31 Mar 2016 15:54
Last Modified: 31 Mar 2016 15:54
URI: http://eprints.kingston.ac.uk/id/eprint/34556

Actions (Repository Editors)

Item Control Page Item Control Page