4 documents found, page 1 of 1
Natural abenquines and synthetic analogues: Preliminary exploration of their cy...
Nain-Perez, Amalyn; Barbosa, Luiz C.A.; Rodríguez-Hernández, Diego; Kramell, Annemarie E.; Heller, Lucie; Csuk, RenéIn this study, we explore the cytotoxic activity of four natural abenquines (2a–d) and fourteen synthetic analogues (2e–j and 3a–h) against a panel of six human cancer cell lines using a SRB assay. It was found that most of the compounds revealed higher levels of cytotoxic activities than naturally occurring abenquines. The analogues carrying ethylpyrrolidinyl and ethylpyrimidinyl with either an acetyl group (2...
Novel hederagenin–triazolyl derivatives as potential anti-cancer agents
Rodríguez-Hernández, Diego; Demuner, Antonio J.; Barbosa, Luiz C.A.; Heller, Lucie; Csuk, RenéA series of novel aryl-1H-1,2,3-triazol-4-yl methylester and amide derivatives of the natural product hederagenin was synthesized aiming to develop new antitumor agents, using Huisgen 1,3-dipolar cycloaddition reactions, with yields between 35% and 95%. The structures of all derivatives (2–31) were confirmed by MS, IR, ^1H NMR and ^13C NMR spectroscopic data. The cytotoxic activities of all compounds were scree...
Leishmanicidal and cytotoxic activity of hederagenin-bistriazolyl derivatives
Rodríguez-Hernández, Diego; Barbosa, Luiz C.A.; Demuner, Antonio J.; Nain-Perez, Amalyn; Ferreira, Sebastião R.; Fujiwara, Ricardo T.Aiming to obtain new potent leishmanicidal and cytotoxic compounds from natural sources, the triterpene hederagenin was converted into several new 1,2,3-triazolyl derivatives tethered at C-23 and C-28. For this work hederagenin was isolated from fruits of Sapindus saponaria and reacted with propargyl bromide to afford as a major product bis-propargylic derivative 1 in 74%. Submitting this compound to Huisgen 1,...
Hederagenin as a triterpene template for the development of new antitumor compo...
Rodríguez-Hernández, Diego; Demuner, Antonio J.; Barbosa, Luiz C.A.; Csuk, René; Heller, LucieIn 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 ...