Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 134, Issue -, Pages 34-42Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2017.04.009
Keywords
Gallium (III); Thiosemicarbazone; Anti-cancer mechanism; Cell cycle; Cell apoptosis
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Funding
- National Nature Science Foundations of China [81571812]
- Priority Academic Program Development of Jiangsu Higher Education Institutions [1107047002]
- Hydron contact lens co., LTD [8507040152]
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Two types of 2-pyridinecarboxaldehyde thiosemicarbazones Ga(III) complexes, which are 2:1 and 1:1 ligand/Ga(III) complexes, were synthesized and determined by X-ray single crystal diffraction. The antiproliferative activity of these Ga(III) complexes have been examined to illuminate the structure-activity relationships essential to form Ga(III) complexes with remarkable anticancer activity. In addition, Ga(III) complexes where the metal/ligand ratio was 1:1 (C4) had observably higher antiproliferative activity than 1:2 (C3). Ga(III) complexes caused a marked increase of caspase-3 and 9 activity in NCI-H460 cells compared to the metal free ligand. Caspase activation was somewhat mediated by the release of Cyt C from mitochondria after incubation with selected agents. Both types of Ga(III) complexes showed more effective in inhibition of the G1/S transition than the ligand alone. (C) 2017 Elsevier Masson SAS. All rights reserved.
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