In:
Medicinal Chemistry, Bentham Science Publishers Ltd., Vol. 16, No. 1 ( 2020-01-16), p. 78-92
Abstract:
In order to discover new agents for chemotherapy with improved properties
compared to the existing agents and bearing in mind the fact that some Pd complexes possess better antitumor activity and exhibit less kidney toxicity compared to cisplatin, a series of novel
square-planar palladium(II) complexes [Pd (L)2] (3a-f) with O,O bidentate ligands [L = ethyl 2-
hydroxy-alkyl(aryl)-4-oxo-2-butenoate] were synthesized. Methods: All complexes were characterized by spectral (UV-Vis, IR, NMR, ESI-MS) and X-ray
analysis and examined for their cytotoxic effect on human cancer cell lines HeLa and MDA-MB 231 and normal fibroblasts (MRC-5). Fluorescence spectroscopic method was used for investigations
of the interactions between CT-DNA or bovine serum albumin (BSA) and complex 3c. Viscosity measurements and molecular docking study were performed to confirm the mode of interactions
between DNA and BSA and complex 3c. Results: Complexes that showed the best results, 3c, 3d, and 3e, were placed under further investigations.
Selected complexes induced apoptosis and cell cycle arrest in HeLa and MDA-MB 231 cells. Low concentrations of 3c and 3e showed strong to moderate synergism with low concentrations
of cisplatin. The interaction of 3d with cisplatin was antagonistic in all used concentrations, but low IC50 value indicates its usefulness as a single cytotoxic agent. It was also noted that the
change of viscosity is more pronounced in DNA solution after addition of complex 3c. Conclusion: Obtained results indicate that the novel palladium(II) complexes have the potential to
become candidates for treatment in anticancer therapy.
Type of Medium:
Online Resource
ISSN:
1573-4064
DOI:
10.2174/1573406415666190128095732
Language:
English
Publisher:
Bentham Science Publishers Ltd.
Publication Date:
2020
SSG:
15,3
