Synthesis and anticancer activities of some novel 2-(benzo[d]thiazol-2-yl)-8-substituted-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones
| Autor: | Helena Carla Castro, Raisa da R. Reis, Carlos Rangel Rodrigues, Letícia V. Costa-Lotufo, Alessandra Mendonça Teles de Souza, Natasha C. de Carvalho, Raquel Carvalho Montenegro, Cláudia Pessoa, José Delano Barreto Marinho Filho, Thatyana R. A. Vasconcelos, Ana Jérsia Araújo, Maria Cecília B. V. de Souza, Vitor F. Ferreira, Manoel Odorico de Moraes, Elisa Carvalho Azevedo |
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| Rok vydání: | 2011 |
| Předmět: |
Pharmacology
Chemistry Stereochemistry Organic Chemistry Antineoplastic Agents Biological activity General Medicine medicine.disease Hemolysis Chemical synthesis In vitro Mice Leukemia Cell culture Cell Line Tumor Drug Discovery Toxicity Quinolines medicine Animals Humans Doxorubicin Cytotoxicity medicine.drug |
| Zdroj: | European Journal of Medicinal Chemistry. 46:1448-1452 |
| ISSN: | 0223-5234 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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