Molecules 2012, 17(5), 6100-6113; doi:10.3390/molecules17056100
Article

Synthesis and Evaluation of New β-Carboline-3-(4-benzylidene)-4H-oxazol-5-one Derivatives as Antitumor Agents

1, 2, 2, 2, 2, 3, 1 and 1,* email
Received: 5 April 2012; in revised form: 5 May 2012 / Accepted: 7 May 2012 / Published: 21 May 2012
(This article belongs to the Section Medicinal Chemistry)
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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.
Keywords: b-carboline; 4H-oxazol-5-one; cytotoxic activity; antimicrobial activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Savariz, F.C.; Foglio, M.A.; de Carvalho, J.E.; Ruiz, A.L.T.G.; Duarte, M.C.T.; da Rosa, M.F.; Meyer, E.; Sarragiotto, M.H. Synthesis and Evaluation of New β-Carboline-3-(4-benzylidene)-4H-oxazol-5-one Derivatives as Antitumor Agents. Molecules 2012, 17, 6100-6113.

AMA Style

Savariz FC, Foglio MA, de Carvalho JE, Ruiz ALTG, Duarte MCT, da Rosa MF, Meyer E, Sarragiotto MH. Synthesis and Evaluation of New β-Carboline-3-(4-benzylidene)-4H-oxazol-5-one Derivatives as Antitumor Agents. Molecules. 2012; 17(5):6100-6113.

Chicago/Turabian Style

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. 2012. "Synthesis and Evaluation of New β-Carboline-3-(4-benzylidene)-4H-oxazol-5-one Derivatives as Antitumor Agents." Molecules 17, no. 5: 6100-6113.


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