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Synthesis and Evaluation of New β-Carboline-3-(4-benzylidene)-4H-oxazol-5-one Derivatives as Antitumor Agents

2012; Multidisciplinary Digital Publishing Institute; Volume: 17; Issue: 5 Linguagem: Inglês

10.3390/molecules17056100

1433-1373

Franciele Cristina Savariz, Mary Ann Foglio, João Ernesto de Carvalho, Ana Lúcia Tasca Góis Ruiz, Marta Cristina Teixeira Duarte, Maurício Ferreira da Rosa, Emerson Meyer, María Helena Sarragiotto,

Synthesis and Reactions of Organic Compounds

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.