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

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

  • Eur J Med Chem. 2011 Apr;46(4):1448-52. doi: 10.1016/j.ejmech.2011.01.066.
Raísa da R Reis 1,  Elisa C Azevedo,  Maria Cecília B V de Souza,  Vitor Francisco Ferreira,  Raquel C Montenegro,  Ana Jérsia Araújo,  Cláudia Pessoa,  Letícia V Costa-Lotufo,  Manoel O de Moraes,  José D B M Filho,  Alessandra M T de Souza,  Natasha C de Carvalho,  Helena C Castro,  Carlos R Rodrigues,  Thatyana R A Vasconcelos
Affiliations

Affiliation

  • 1 Universidade Federal Fluminense, Instituto de Química, Departamento de Química Orgânica, Outeiro de São João Batista, Centro, Niterói 24020-141, RJ, Brazil.
PMID: 21334795 DOI: 10.1016/j.ejmech.2011.01.066
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.

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