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Type: Artigo de periódico
Title: Synthesis And Antitumoral Activity Of Novel 3-(2-substituted-1,3,4-oxadiazol-5-yl) And 3-(5-substituted-1,2,4-triazol-3-yl) β-carboline Derivatives
Author: Formagio A.S.N.
Tonin L.T.D.
Foglio M.A.
Madjarof C.
de Carvalho J.E.
da Costa W.F.
Cardoso F.P.
Sarragiotto M.H.
Abstract: Several novel 1-substituted-phenyl β-carbolines bearing the 2-substituted-1,3,4-oxadiazol-5-yl and 5-substituted-1,2,4-triazol-3-yl groups at C-3 were synthesized and evaluated for their in vitro anticancer activity. The assay results pointed thirteen compounds with growth inhibition effect (GI 50 < 100 μM) for all eight different types of human cancer cell lines tested. The β-carbolines 7a and 7h, bearing the 3-(2-metylthio-1,3,4-oxadiazol-5-yl) group, displayed high selectivity and potent anticancer activity against ovarian cell line with GI 50 values lying in the nanomolar concentration range (GI 50 = 10 nM for both compounds). The 1-(N,N-dimethylaminophenyl)-3-(5-thioxo-1,2,4-triazol-3-yl) β-carboline (8g) was the most active compound, showing particular effectiveness on lung (GI 50 = 0.06 μM), ovarian and renal cell lines. The potent anticancer activity presented for synthesized compounds 7a, 7h, and 8g, together with their easiness of synthesis, makes these compounds promising anticancer agents. © 2008 Elsevier Ltd. All rights reserved.
Citation: Bioorganic And Medicinal Chemistry. , v. 16, n. 22, p. 9660 - 9667, 2008.
Rights: fechado
Identifier DOI: 10.1016/j.bmc.2008.10.008
Date Issue: 2008
Appears in Collections:Unicamp - Artigos e Outros Documentos

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