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Synthesis and anticancer activities of some novel 2-(benzo[d]thiazol-2-yl)-8-substituted-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones

2011; Elsevier BV; Volume: 46; Issue: 4 Linguagem: Inglês

10.1016/j.ejmech.2011.01.066

1768-3254

Raísa da R. Reis, Elisa Carvalho Azevedo, Maria Cecília B. V. de Souza, Vı́tor F. Ferreira, Raquel Carvalho Montenegro, Ana Jérsia Araújo, Cláudia Pessoa, Letícia V. Costa‐Lotufo, Manoel Odorico de Moraes, José Delano Barreto Marinho Filho, Alessandra Mendonça Teles de Souza, Natasha C. de Carvalho, Helena Carla Castro, Carlos Rangel Rodrigues, T.R.A. Vasconcelos,

Multicomponent Synthesis of Heterocycles

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 IC50 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.