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Synthesis and Evaluation of New β-Carboline-3-(4-benzylidene)-4H-oxazol-5-one Derivatives as Antitumor Agents
Departamento de Química, Centro de Ciências Exatas, Universidade Estadual de Maringá, Av. Colombo, 5790, Maringá, 87020-900 PR, Brazil
Centro Pluridisciplinar de Pesquisas Químicas, Biológicas e Agrícolas (CPQBA), Universidade Estadual de Campinas, 6171, Campinas, 13083-970 SP, Brazil
Centro de Engenharias e Ciências Exatas, Universidade Estadual do Oeste do Paraná, Rua da Faculdade, 645, Toledo, 85903-000 PR, Brazil
* Author to whom correspondence should be addressed.
Received: 5 April 2012; in revised form: 5 May 2012 / Accepted: 7 May 2012 / Published: 21 May 2012
Abstract: In the present work, we report the synthesis and in vitro anticancer and antimicrobial activity evaluation of a new series of 1-substituted-β-carboline derivatives bearing a 4-benzylidene-4H-oxazol-5-one unity at C-3. The compound 2-[1-(4-methoxyphenyl)-9H-β-carbolin-3-yl]-4-(benzylidene)-4H-oxazol-5-one (11) was the most active derivative, exhibiting a potent cytotoxic activity against glioma (U251), prostate (PC-3) and ovarian (OVCAR-03) cancer cell lines with IC50 values of 0.48, 1.50 and 1.07 µM, respectively. An in silico study of the ADME properties of the novel synthesized β-carboline derivatives was also performed.
Keywords: b-carboline; 4H-oxazol-5-one; cytotoxic activity; antimicrobial activity
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MDPI and ACS Style
Savariz, F.C.; Foglio, M.A.; de Carvalho, J.E.; Ruiz, A.L.T.G.; Duarte, M.C.T.; da Rosa, M.F.; Meyer, E.; Sarragiotto, M.H. Synthesis and Evaluation of New β-Carboline-3-(4-benzylidene)-4H-oxazol-5-one Derivatives as Antitumor Agents. Molecules 2012, 17, 6100-6113.
Savariz FC, Foglio MA, de Carvalho JE, Ruiz ALTG, Duarte MCT, da Rosa MF, Meyer E, Sarragiotto MH. Synthesis and Evaluation of New β-Carboline-3-(4-benzylidene)-4H-oxazol-5-one Derivatives as Antitumor Agents. Molecules. 2012; 17(5):6100-6113.
Savariz, Franciele Cristina; Foglio, Mary Ann; de Carvalho, João Ernesto; Ruiz, Ana Lúcia T. G.; Duarte, Marta C. T.; da Rosa, Mauricio Ferreira; Meyer, Emerson; Sarragiotto, Maria Helena. 2012. "Synthesis and Evaluation of New β-Carboline-3-(4-benzylidene)-4H-oxazol-5-one Derivatives as Antitumor Agents." Molecules 17, no. 5: 6100-6113.