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 |
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| Authors: | José Agustín Quincoces Suarez Daniela Gonçales Rando Reginaldo Pereira Santos Carolina Passarelli Gonçalves Elizabeth Ferreira João Ernesto de Carvalho Luciana Kohn Durvanei Augusto Maria Fernanda Faião-Flores Dirk Michalik Maria Cristina Marcucci Christian Vogel |
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| Institution: | 1. Laboratory of Organic Synthesis, Universidade Bandeirante de São Paulo (UNIBAN), São Paulo, Brazil;2. LAPEN, Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo (USP), São Paulo, Brazil;3. Division of Pharmacology and Toxicology, Multidisciplinary Center for Chemical, Biological and Agricultural, State University of Campinas, UNICAMP, Campinas, Brazil;4. Laboratory of Biochemistry and Biophysics, Butantan Institute, São Paulo, Brazil;5. Leibniz-Institut für Katalyse, Rostock, Germany;6. Laboratory of Natural Products, Universidade Bandeirante de São Paulo (UNIBAN), São Paulo, Brazil;7. Institut für Chemie, University Rostock, Germany |
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| 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 IC50 values ?2.3 μM for all human cancer cell lines. Intraperitoneal acute administration of compound 1 and 2 showed very low toxicity rate. |
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