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Issue 4, 2017
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Design and synthesis of cenocladamide analogues and their evaluation against breast cancer cell lines

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Abstract

This work describes the total synthesis of the alkaloid cenocladamide and a concise library of nine structural analogues aiming at their evaluation against the breast cancer cell line MDA-MB-231. The most promising compound (3; IC50 = 6.6 μM) was also evaluated in a panel of seven breast cancer cell lines and two non-tumorigenic cell lines. We further conducted an initial investigation on the mechanism of action of analogue 3, which lacks the endocyclic double bond when compared to cenocladamide. The present study presents the discovery of a cenocladamide analogue with interesting cytotoxic activity, which could be useful for further optimization towards new chemotherapeutic agents for breast cancer treatment.

Graphical abstract: Design and synthesis of cenocladamide analogues and their evaluation against breast cancer cell lines

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Publication details

The article was received on 14 Oct 2016, accepted on 21 Nov 2016 and first published on 25 Nov 2016


Article type: Research Article
DOI: 10.1039/C6MD00577B
Citation: Med. Chem. Commun., 2017,8, 755-766
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    Design and synthesis of cenocladamide analogues and their evaluation against breast cancer cell lines

    C. C. F. Santos, L. S. Paradela, L. F. T. Novaes, S. M. G. Dias and J. C. Pastre, Med. Chem. Commun., 2017, 8, 755
    DOI: 10.1039/C6MD00577B

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