Molecules p. 6100 - 6113 (2012)
Update date:2022-08-05
Topics:
Savariz, Franciele Cristina
Foglio, Mary Ann
De Carvalho, Joao Ernesto
Ruiz, Ana Lucia T.G.
Duarte, Marta C.T.
Da Rosa, Mauricio Ferreira
Meyer, Emerson
Sarragiotto, Maria Helena
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.
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(2012)