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

• DOI: 10.1016/j.ejmech.2011.01.066
• Publication Date: 2011-02-04T09:15:33Z
• Authors: Raísa da R. Reis; Elisa C. Azevedo; Maria Cecília B.V...; Vitor Francisco F...; Raquel C. Montenegro; Ana Jérsia Araújo; Cláudia Pessoa; Letícia V. Costa-...; Manoel O. de Moraes; José D.B.M. Filho; Alessandra M.T. d...; Natasha C. de Car...; Helena C. Castro; Carlos R. Rodrigues; Thatyana R.A. Vas...
• Keywords: Mice; Cell Line, Tumor; Quinolines; Animals; Humans; Antineoplastic Agents; Hemolysis; 01 natural sciences; 3. Good health; 0104 chemical sciences

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.