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Bioorg Med Chem. 2013 Nov 15;21(22):6920-8. doi: 10.1016/j.bmc.2013.09.030. Epub 2013 Sep 19.

Quinazolinecarboline alkaloid evodiamine as scaffold for targeting topoisomerase I and sirtuins.

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  • 1Dipartimento di Chimica, Universit√† degli Studi di Milano, Via Golgi 19, 20133 Milano, Italy.

Abstract

This paper reports the synthesis of a series of evodiamine derivatives. We assayed the ability to inhibit cell growth on three human tumour cell lines (H460, MCF-7 and HepG2) and we evaluated the capacity to interfere with the catalytic activity of topoisomerase I both by the relaxation assay and the occurrence of the cleavable complex. Moreover, whose effect on sirtuins 1, 2 and 3 was investigated. Finally, molecular docking analyses were performed in an attempt to rationalize the biological results.

Copyright © 2013 Elsevier Ltd. All rights reserved.

KEYWORDS:

Evodiamine; Quinazolinecarboline alkaloids; Sirtuins; Topoisomerase I; enantiomer; ent; epi; epimer

PMID:
24103429
[PubMed - indexed for MEDLINE]
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