| Full text | |
| Author(s): Show less - |
Quincoces Suarez, Jose Agustin
[1]
;
Rando, Daniela Goncales
[2]
;
Santos, Reginaldo Pereira
[1]
;
Goncalves, Carolina Passarelli
[1]
;
Ferreira, Elizabeth
[2]
;
de Carvalho, Joao Ernesto
[3]
;
Kohn, Luciana
[3]
;
Maria, Durvanei Augusto
[4]
;
Faiao-Flores, Fernanda
[4]
;
Michalik, Dirk
[5]
;
Marcucci, Maria Cristina
[6]
;
Vogel, Christian
[7]
Total Authors: 12
|
| Affiliation: | [1] Univ Bandeirante Sao Paulo UNIBAN, Organ Synth Lab, Sao Paulo - Brazil
[2] Univ Sao Paulo USP, LAPEN, Dept Pharm, Fac Pharmaceut Sci, Sao Paulo - Brazil
[3] Univ Estadual Campinas, UNICAMP, Div Pharmacol & Toxicol, Multidisciplinary Ctr Chem Biol & Agr, Campinas - Brazil
[4] Butantan Inst, Biochem & Biophys Lab, Sao Paulo - Brazil
[5] Leibniz Inst Katalyse, Rostock - Germany
[6] Univ Bandeirante Sao Paulo UNIBAN, Lab Nat Prod, Sao Paulo - Brazil
[7] Univ Rostock, Inst Chem, D-2500 Rostock 1 - Germany
Total Affiliations: 7
|
| Document type: | Journal article |
| Source: | Bioorganic & Medicinal Chemistry; v. 18, n. 17, p. 6275-6281, SEP 1 2010. |
| Web of Science Citations: | 15 |
| 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. (AU) | |