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Revista Colombiana de Ciencias Químico - Farmacéuticas
versão impressa ISSN 0034-7418versão On-line ISSN 1909-6356
Resumo
DOS ANJOS SANTOS, Victória Laysna et al. Hydrazones derived from natural aldehydes: in vitro cytotoxic evaluation and in silico pharmacokinetic predictions. Rev. colomb. cienc. quim. farm. [online]. 2021, vol.50, n.1, pp.217-235. Epub 05-Nov-2021. ISSN 0034-7418. https://doi.org/10.15446/rcciquifa.v50n1.91232.
Introduction:
Recent research has reported the cytotoxic potential of hydrazones against various strains of cancer cells.
Aim:
To evaluate the anticancer activity in vitro and the pharmacokinetic profile of six synthesized hydrazonic compounds, identified as vanillin 1-phthalazinylhydrazone (VAN-1); 2,4-dinitrophenylhydra-zone vanillin (VAN-2); phenylhydrazone cinnamaldehyde (CIN-1); isonicotinoyl hydrazone cinnamaldehyde (CIN-2); cinnamaldehyde 1-phthalazinylhydrazone (CIN-3); and 2,4-dinitrophenylhydrazone cinnamaldehyde (CIN-4). The cytotoxic activity was evaluated against four strains of cancer cells.
Methodology:
The pharmacokinetic parameters of absorption, distribution, metabolism, excretion, and toxicity (ADME/T) of the hydrazones were evaluated using the PreADMET program.
Results:
Hydrazones derived from cinnamaldehyde (CIN-1 and CIN-2) showed high cytotoxic activity against leukemic (HL-60) and glioblastomas (SF-295) cell lines. The pharmacokinetic profile of the hydrazones showed that, in general, the hydrazones presented satisfactory characteristics of ADME/T. In addition, it was observed that CIN-2 presented the most promising in silico profile, showing high intestinal absorption, desirable distribution profile related to plasma protein binding, adequate renal excretion, and low toxicity. The ADME/T profile of the CIN-1 compound highlighted its potential as a promising antineoplastic agent with action of the CNS, more specifically against glioblastomas.
Palavras-chave : Antineoplastic drugs; cancer; molecular hybridization; phenylhydrazones.