1. Synthesis and anticancer activities of some novel 2-(benzo[d]thiazol-2-yl)-8-substituted-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones.
- Author
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Reis Rda R, Azevedo EC, de Souza MC, Ferreira VF, Montenegro RC, Araújo AJ, Pessoa C, Costa-Lotufo LV, de Moraes MO, Filho JD, de Souza AM, de Carvalho NC, Castro HC, Rodrigues CR, and Vasconcelos TR
- Subjects
- Animals, Antineoplastic Agents chemistry, Cell Line, Tumor, Hemolysis drug effects, Humans, Mice, Quinolines chemistry, Antineoplastic Agents chemical synthesis, Antineoplastic Agents pharmacology, Quinolines chemical synthesis, Quinolines pharmacology
- Abstract
A series of 2-(benzo[d]thiazol-2-yl)-8-substituted-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones (3a-g) have been synthesized and evaluated for their in vitro antiproliferative activities against four human cancer cell lines: MDA-MB-435 (breast), HL-60 (leukemia), HCT-8 (colon) and SF-295 (central nervous system). The results showed that the compounds 3b (2-(benzo[d]thiazol-2-yl)-8-methyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-one) and 3c (2-(benzo[d]thiazol-2-yl)-8-bromo-2H-pyrazolo[4,3-c]quinolin-3(5H)-one) exhibited good cytotoxicity for three cell lines with IC(50) values lower than 5 μg/mL. Analysis of theoretical toxicity risks have shown medium tumorigenic and irritant risks related to 3b and 3c in contrast to doxorubicin, the positive control., (Copyright © 2011 Elsevier Masson SAS. All rights reserved.)
- Published
- 2011
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