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Synthesis and evaluation of new ?-carboline-3-(4-benzylidene)-4H-oxazol-5-one derivatives as antitumor agents.

ABSTRACT: In the present work, we report the synthesis and in vitro anticancer and antimicrobial activity evaluation of a new series of 1-substituted-?-carboline derivatives bearing a 4-benzylidene-4H-oxazol-5-one unity at C-3. The compound 2-[1-(4-methoxyphenyl)-9H-?-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 ?-carboline derivatives was also performed.

SUBMITTER: Savariz FC

PROVIDER: S-EPMC6268609 | biostudies-literature | 2012 May

REPOSITORIES: biostudies-literature

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Synthesis and evaluation of new β-carboline-3-(4-benzylidene)-4H-oxazol-5-one derivatives as antitumor agents.

Savariz Franciele Cristina FC Foglio Mary Ann MA de Carvalho João Ernesto JE Ruiz Ana Lúcia T G AL Duarte Marta C T MC da Rosa Mauricio Ferreira MF Meyer Emerson E Sarragiotto Maria Helena MH

Molecules (Basel, Switzerland) 20120521 5

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 1.0 ...[more]

PMID: 22614863

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