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Type: Artigo de periódico
Title: Synthesis of methoxylated goniothalamin, aza-goniothalamin and gamma-pyrones and their in vitro evaluation against human cancer cells
Author: Barcelos, RC
Pastre, JC
Caixeta, V
Vendramini-Costa, DB
de Carvalho, JE
Pilli, RA
Abstract: The present work describes the preparation of three novel series of compounds based on the structure of goniothalamin, a natural styryl lactone which has been found to display cytotoxic and antiproliferative activities against a variety of cancer cell lines. A focused library of 29 novel goniothalamin analogues was prepared and evaluated against seven human cancer cell lines. While the gamma-pyrones and the azagoniothalamin analogues were less potent than the lead compound, 2,4-dimethoxy analogue 88 has shown to be more potent in vitro than goniothalamin against all cancer cell lines evaluated. Furthermore, it was more potent than doxorubicin against NCI-ADR/RES, OVCAR-03 and HT-29 while being less toxic to human keratinocytes (HaCat). The 3,5-dimethoxy analogue 90 and 2,4,5-trimethoxy analogue 92 also displayed promising antiproliferative activity when compared to goniothalamin ( 1). These results provide new elements for the design and synthesis of novel representatives of this family of natural compounds. (C) 2012 Elsevier Ltd. All rights reserved.
Subject: Goniothalamin
Cancer cells
Antiproliferative activity
Country: Inglaterra
Editor: Pergamon-elsevier Science Ltd
Citation: Bioorganic & Medicinal Chemistry. Pergamon-elsevier Science Ltd, v. 20, n. 11, n. 3635, n. 3651, 2012.
Rights: fechado
Identifier DOI: 10.1016/j.bmc.2012.03.059
Date Issue: 2012
Appears in Collections:Unicamp - Artigos e Outros Documentos

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