1. Synthesis and evaluation of new β-carboline-3-(4-benzylidene)-4H-oxazol-5-one derivatives as antitumor agents.
- Author
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Savariz FC, Foglio MA, de Carvalho JE, Ruiz AL, Duarte MC, da Rosa MF, Meyer E, and Sarragiotto MH
- Subjects
- Anti-Infective Agents chemical synthesis, Anti-Infective Agents chemistry, Anti-Infective Agents pharmacology, Antineoplastic Agents chemistry, Bacteria drug effects, Carbolines chemistry, Cell Line, Tumor, Cell Survival drug effects, Fungi drug effects, Humans, Inhibitory Concentration 50, Oxazoles chemistry, Antineoplastic Agents chemical synthesis, Antineoplastic Agents pharmacology, Carbolines chemical synthesis, Carbolines pharmacology, Oxazoles chemical synthesis, Oxazoles pharmacology
- 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.
- Published
- 2012
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