title: Synthesis and anticancer activities of some novel 2-(benzo[d]thiazol-2-yl)-8-substituted-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones.
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.
authors.affiliation: Universidade Federal Fluminense, Instituto de Química, Departamento de Química Orgânica, Outeiro de São João Batista, Centro, Niterói 24020-141, RJ, Brazil.
authors.forename: Raísa da R
authors.initials: Rda R
authors.lastname: Reis
authors.forename: Elisa C
authors.initials: EC
authors.lastname: Azevedo
authors.forename: Maria Cecília B V
authors.initials: MC
authors.lastname: de Souza
authors.forename: Vitor Francisco
authors.initials: VF
authors.lastname: Ferreira
authors.forename: Raquel C
authors.initials: RC
authors.lastname: Montenegro
authors.forename: Ana Jérsia
authors.initials: AJ
authors.lastname: Araújo
authors.forename: Cláudia
authors.initials: C
authors.lastname: Pessoa
authors.forename: Letícia V
authors.initials: LV
authors.lastname: Costa-Lotufo
authors.forename: Manoel O
authors.initials: MO
authors.lastname: de Moraes
authors.forename: José D B M
authors.initials: JD
authors.lastname: Filho
authors.forename: Alessandra M T
authors.initials: AM
authors.lastname: de Souza
authors.forename: Natasha C
authors.initials: NC
authors.lastname: de Carvalho
authors.forename: Helena C
authors.initials: HC
authors.lastname: Castro
authors.forename: Carlos R
authors.initials: CR
authors.lastname: Rodrigues
authors.forename: Thatyana R A
authors.initials: TR
authors.lastname: Vasconcelos
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D051379:Mice; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011804:Quinolines