Hederagenin as a triterpene template for the development of new antitumor compounds

dc.creatorRodríguez-Hernández, Diego
dc.creatorDemuner, Antonio J.
dc.creatorBarbosa, Luiz C.A.
dc.creatorCsuk, René
dc.creatorHeller, Lucie
dc.date2018-05-09T18:21:17Z
dc.date2018-05-09T18:21:17Z
dc.date2015-11-13
dc.date.accessioned2023-09-27T21:03:47Z
dc.date.available2023-09-27T21:03:47Z
dc.identifier02235234
dc.identifierhttps://doi.org/10.1016/j.ejmech.2015.10.006
dc.identifierhttp://www.locus.ufv.br/handle/123456789/19427
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8953808
dc.descriptionIn this study, a series of novel C-28 esters and amides derivatives of hederagenin (He) were designed and synthesized in attempt to develop potent antitumor agents. Their structures were confirmed by MS, IR, 1H NMR and ^13C NMR spectroscopic analyses and their cytotoxic activities were screened in SRB assays using a panel of six human cancer cell lines. Although most of the compounds displayed moderate to high levels of cytotoxic activity they were all more potent than the natural product He. The most active compounds had either an ethylpyrimidinyl (27) or an ethylpyrrolidinyl (28) substituent, with EC50 in the range of 1.1–6.5 μM for six human cancer cell lines. Notably, this corresponds to an approximately 30-fold times greater potency than He.
dc.formatpdf
dc.formatapplication/pdf
dc.languageeng
dc.publisherEuropean Journal of Medicinal Chemistry
dc.relationv. 105, p. 57-62, nov. 2015
dc.rightsElsevier Masson SAS.
dc.subjectSapindus saponaria
dc.subjectPentacyclic triterpenes
dc.subjectHederagenin derivatives
dc.subjectSRB assay
dc.subjectFolk medicinal plant
dc.titleHederagenin as a triterpene template for the development of new antitumor compounds
dc.typeArtigo


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