Please use this identifier to cite or link to this item: http://hdl.handle.net/10553/120006
Title: Guanidine Derivatives Containing the Chalcone Skeleton Are Potent Antiproliferative Compounds against Human Leukemia Cells
Authors: Estévez Sarmiento,Francisco 
Saavedra Díaz, Ester Gloria 
Brouard Martín,Ignacio 
Peyrac, Jesús
Hernández-Garcés, Judith
García, Celina
Quintana Aguiar, José Martín 
Estévez Rosas, Francisco Jesús 
UNESCO Clasification: 32 Ciencias médicas
320713 Oncología
320102 Genética clínica
Keywords: Apoptosis
Caspases
Cell Cycle
Cytotoxicity
Guanidines, et al
Issue Date: 2022
Journal: International Journal of Molecular Sciences 
Abstract: In this study, we investigated the effects of eleven synthetic guanidines containing the 1,3-diphenylpropenone core on the viabilities of six human cancer cells. The most cytotoxic compound against human cancer cells of this series contains a N-tosyl group and a N-methylpiperazine moiety 6f. It was cytotoxic against leukemia cells (U-937, HL-60, MOLT-3, and NALM-6) with significant effects against Bcl-2-overexpressing U-937/Bcl-2 cells as well as the human melanoma SK-MEL-1 cell line. It exhibited low cytotoxicity against quiescent or proliferating human peripheral blood mononuclear cells. The IC50 value for the leukemia U-937 cells was 1.6 ± 0.6 µM, a similar value to that in the antineoplastic agent etoposide. The guanidine containing a N-phenyl substituent 6i was also as cytotoxic as the guanidine containing the N-tosyl substituent and the N-methylpiperazine group 6f against human U-937 leukemia cells and both synthetic guanidines were potent apoptotic inducers. Cell death was mediated by the activation of the initiator caspase-9 and the executioner caspase-3, and associated with the release of cytochrome c. These synthetic guanidines are potent cytotoxic compounds against several human leukemia cells and even the human melanoma cell line SK-MEL-1 and might be useful in the development of new strategies in the fight against cancer.
URI: http://hdl.handle.net/10553/120006
ISSN: 1422-0067
DOI: 10.3390/ijms232415518
Source: International journal of molecular sciences [EISSN 1422-0067], v. 23 (24), 15518, (Diciembre 2022)
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