3 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...
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,...
Tailoring natural abenquines to inhibit the photosynthetic electron transport t...
Nain-Perez, Amalyn; Barbosa, Luiz C. A.; Maltha, Celia R. A.; Giberti, Samuele; Forlani, GiuseppeAbenquines are natural N-acetylaminobenzoquinones bearing amino acid residues, which act as weak inhibitors of the photosynthetic electron transport chain. Aiming to exploit the abenquine scaffold as a model for the synthesis of new herbicides targeting photosynthesis, 14 new analogues were prepared by replacing the amino acid residue with benzylamines and the acetyl with different acyl groups. The synthesis wa...