Synthesis and Evaluation of New β-Carboline-3-(4-benzylidene)-<em>4H</em>-oxazol-5-one Derivatives as Antitumor Agents
oleh: Maria Helena Sarragiotto, Emerson Meyer, Marta C. T. Duarte, Mauricio Ferreira da Rosa, João Ernesto de Carvalho, Ana Lúcia T. G. Ruiz, Mary Ann Foglio, Franciele Cristina Savariz
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2012-05-01 |
Deskripsi
In the present work, we report the synthesis and<em> in vitro</em> anticancer and antimicrobial activity evaluation of a new series of 1-substituted-β-carboline derivatives<strong> </strong>bearing a 4-benzylidene-<em>4H-</em>oxazol-5-one unity at C-3. The compound 2-[1-(4-methoxyphenyl)-<em>9H</em>-β-carbolin-3-yl]-4-(benzylidene)<em>-4H-</em>oxazol-5-one (<strong>11</strong>) was the most active derivative, exhibiting a potent cytotoxic activity against glioma (U251), prostate (PC-3) and ovarian (OVCAR-03) cancer cell lines with IC<sub>50</sub> values of 0.48, 1.50 and 1.07 µM, respectively. An <em>in silico</em> study of the ADME properties of the novel synthesized β-carboline derivatives was also performed.