Benites, Julio
[Universidad Arturo Prat]
Valderrama, Jaime A
[Pontificia Universidad Catolica de Chile]
Bettega, Karina
[Universidade Federal de Santa Catarina]
Pedrosa, Rozangela Curi
[Universidade Federal de Santa Catarina]
Buc Calderon, Pedro
[UCL]
Verrax, Julien
[UCL]
Several members of the phenylamino-1,4-naphthoquinone series were prepared in order to investigate structure-activity relationships (SAR) and to explore the antitumor effects associated with this scaffold. The cytotoxic effects of the aminoquinones (EC50) against a panel of cancer cell lines (MCF7, DU145 and T24 cells) and healthy fibroblasts (BALB/3T3) were assessed in vitro using the MTT reduction assay 48 h after drug exposure. SAR analysis of the aminonaphthoquinone series showed that insertion of a chlorine atom in the acceptor quinone nucleus and/or insertion of a methyl group at the nitrogen atom of the donor phenylamino group induced significant changes in cytotoxic activity. Quinones 7 and 9, which exhibited the highest selective indexes (5.73 and 6.29, respectively), were further characterized using the following assays: Colony formation, caspase-3 activity, and ATP content. The results showed that aminoquinone 7 strongly influenced ATP levels and impaired the proliferative capacity of T24 cells without activating caspase-3.
Référence bibliographique |
Benites, Julio ; Valderrama, Jaime A ; Bettega, Karina ; Pedrosa, Rozangela Curi ; Buc Calderon, Pedro ; et. al. Biological evaluation of donor-acceptor aminonaphthoquinones as antitumor agents.. In: European journal of medicinal chemistry, Vol. 45, no. 12, p. 6052-7 (2010) |
Permalien |
http://hdl.handle.net/2078.1/81657 |