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- Title
Synthesis and Evaluation of New β-Carboline-3-(4-benzylidene)-4H-oxazol-5-one Derivatives as Antitumor Agents.
- Authors
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
- 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.
- Subjects
ANTINEOPLASTIC agents; ANTI-infective agents; BENZYLIDENE compounds; GUAIACOL; OXAZOLES; CHEMICAL derivatives
- Publication
Molecules, 2012, Vol 17, Issue 5, p6100
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules17056100