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Type: Artigo de periódico
Title: Synthesis Of Methoxylated Goniothalamin, Aza-goniothalamin And γ-pyrones And Their In Vitro Evaluation Against Human Cancer Cells.
Author: Barcelos, Rosimeire Coura
Pastre, Julio Cezar
Caixeta, Vanessa
Vendramini-Costa, Débora Barbosa
de Carvalho, João Ernesto
Pilli, Ronaldo Aloise
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 γ-pyrones and the aza-goniothalamin 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.
Subject: Cell Line, Tumor
Cell Proliferation
Drug Design
Drug Screening Assays, Antitumor
Molecular Structure
Small Molecule Libraries
Structure-activity Relationship
Rights: fechado
Identifier DOI: 10.1016/j.bmc.2012.03.059
Date Issue: 2012
Appears in Collections:Artigos e Materiais de Revistas Científicas - Unicamp

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