Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue -, Pages 163-172Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.01.051
Keywords
Hydrazones; Gallium(III) complexes; Crystal structures; Glioma cells; Cytotoxic activity; SAR studies
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Funding
- CNPq
- INCT-INOFAR [Proc. CNPq 573.364/2008-6]
- INCT-CATALISE
- FAPEMIG
- CNEN
- FAPESP (Brazil)
- CONICET (Argentina)
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2-Acetylpyridine-phenylhydrazone (H2AcPh), its para-chlorophenylhydrazone (H2AcpClPh) and para-nitrophenylhydrazone (H2AcpNO(2)Ph) analogues, the corresponding 2-benzoylpyridine-derived hydrazones (H2BzPh, H2BzpClPh and H2BzpNO(2)Ph) and their gallium(III) complexes were assayed for their cytotoxic activity against U87 (expressing wild-type p53 protein) and T98 (expressing mutant p53 protein) glioma cells. IC50 values against both glioma cells and against the MRC5 (human fetal lung fibroblast) lineage were obtained for the hydrazones, but not for their gallium(III) complexes, due to their low solubility. Hydrazones were highly cytotoxic at nanomolar doses against U87 and T98 cells. The therapeutic indexes (TI = IC50MRC5/IC50glioma) were 2-660 for T98 cells and 28-5000 for U87 cells, indicating that the studied hydrazones could be good antitumor drug candidates to treat brain tumors. (C) 2012 Elsevier Masson SAS. All rights reserved.
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