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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

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

Full text
Author(s):
Santos, Carla C. F. ; Paradela, Luciana S. ; Novaes, Luiz F. T. ; Dias, Sandra M. G. ; Pastre, Julio C.
Total Authors: 5
Document type: Journal article
Source: MedChemComm; v. 8, n. 4, p. 755-766, APR 1 2017.
Web of Science Citations: 5
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 mu M) 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. (AU)

FAPESP's process: 15/08199-6 - Application of Dioxiranes in continuous flow, synthesis of Actinoranone and decalin fragment of Azadirachtin
Grantee:Luiz Fernando Toneto Novaes
Support Opportunities: Scholarships in Brazil - Doctorate
FAPESP's process: 14/25770-6 - New frontiers in cross-coupling reactions promoted by palladium: combining enantioselective catalysis, C-H activations, new materials and in flux reactions aiming at high efficiency and sustainability in synthetic processes
Grantee:Carlos Roque Duarte Correia
Support Opportunities: Research Projects - Thematic Grants
FAPESP's process: 14/26378-2 - Development of methodologies and synthetic processes employing a new technological platform: micro and meso reactor assisted synthesis of natural products and derivatives with potential pharmacological activity
Grantee:Júlio Cezar Pastre
Support Opportunities: Research Grants - Young Investigators Grants
FAPESP's process: 14/15968-3 - Understanding the glutaminase functional regulation and the development of inhibitors as new approaches to cancer therapy
Grantee:Sandra Martha Gomes Dias
Support Opportunities: Regular Research Grants