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Type: Artigo de periódico
Title: Synthesis And Antitumor Activity Of Novel 1-substituted Phenyl 3-(2-oxo-1,3,4-oxadiazol-5-yl) β-carbolines And Their Mannich Bases.
Author: Savariz, Franciele Cristina
Foglio, Mary Ann
Ruiz, Ana Lucia T Goes
da Costa, Willian Ferreira
Silva, Marina de Magalhães
Santos, Josué Carinhanha Caldas
Figueiredo, Isis Martins
Meyer, Emerson
de Carvalho, João Ernesto
Sarragiotto, Maria Helena
Abstract: A series of novel 1-(substituted phenyl)-3-(2-oxo-1,3,4-oxadiazol-5-yl) β-carbolines (4a-e) and the corresponding Mannich bases 5-9(a-c) were synthesized and evaluated for their in vitro antitumor activity against seven human cancer cell lines. Compounds of 4a-e series showed a broad spectrum of antitumor activity, with GI50 values lower than 15μM for five cell lines. The derivative 4b, having the N,N-dimethylaminophenyl group at C-1, displayed the highest activity with GI50 in the range of 0.67-3.20μM. A high selectivity and potent activity were observed for some Mannich bases, particularly towards resistant ovarian (NCI-ADR/RES) cell lines (5a, 5b, 6a, 6c and 9b), and ovarian (OVCAR-03) cell lines (5b, 6a, 6c, 9a, 9b and 9c). In addition, the interaction of compound 4b with DNA was investigated by using UV and fluorescence spectroscopic analysis. These studies indicated that 4b interact with ctDNA by intercalation binding.
Subject: 2-oxo-1,3,4-oxadiazole
Antitumor Activity
Mannich Bases
Ctdna Interaction
Citation: Bioorganic & Medicinal Chemistry. v. 22, n. 24, p. 6867-75, 2014-Dec.
Rights: fechado
Identifier DOI: 10.1016/j.bmc.2014.10.031
Date Issue: 2014
Appears in Collections:Unicamp - Artigos e Outros Documentos

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