Please use this identifier to cite or link to this item: http://repositorio.unicamp.br/jspui/handle/REPOSIP/478
Type: Artigo de periódico
Title: New antitumoral agents I: In vitro anticancer activity and in vivo acute toxicity of synthetic 1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadien-3-one and derivatives
Author: SUAREZ, Jose Agustin Quincoces
RANDO, Daniela Goncales
SANTOS, Reginaldo Pereira
GONCALVES, Carolina Passarelli
FERREIRA, Elizabeth
CARVALHO, Joao Ernesto de
KOHN, Luciana
MARIA, Durvanei Augusto
FAIAO-FLORES, Fernanda
MICHALIK, Dirk
MARCUCCI, Maria Cristina
VOGEL, Christian
Abstract: This paper describes a new method for the preparation of 1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadien-3-one 1 and its derivatives 2-5. This set of synthetic compounds exhibited high antitumoral activities regarding in vitro screening against several human tumor cell lines as lung carcinoma NCI-460, melanoma UACC-62, breast MCF-7, colon HT-29, renal 786-O, ovarian OVCAR-03 and ovarian expressing the resistance phenotype for adriamycin NCI-ADR/ RES, prostate PC-3, and leukemia K-562. Compounds were also tested against murine tumor cell line B16F10 melanoma and lymphocytic leukemia L1210 as well as to their effect toward normal macrophages. Specific activity against colon cancer cells HT-29 was observed for all tested compounds and suggests further studies with models of colon cancer. Compounds 1, 2, and 4 showed significant cytotoxic activity with IC(50) values <= 2.3 mu M for all human cancer cell lines. Intraperitoneal acute administration of compound 1 and 2 showed very low toxicity rate. (C) 2010 Elsevier Ltd. All rights reserved.
Subject: Synthesis
Diarylpentadienone derivatives
Cytotoxicity
LD(50) toxicity
Antineoplastic agents
Country: Inglaterra
Editor: PERGAMON-ELSEVIER SCIENCE LTD
Citation: BIOORGANIC & MEDICINAL CHEMISTRY, v.18, n.17, p.6275-6281, 2010
Rights: fechado
Identifier DOI: 10.1016/j.bmc.2010.07.026
Address: http://apps.isiknowledge.com/InboundService.do?Func=Frame&product=WOS&action=retrieve&SrcApp=EndNote&UT=000281203300007&Init=Yes&SrcAuth=ResearchSoft&mode=FullRecord
http://dx.doi.org/10.1016/j.bmc.2010.07.026
Date Issue: 2010
Appears in Collections:CPQBA - Artigos e Outros Documentos

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