In Vitro and In Vivo Biological Activities of Dipicolinate Oxovanadium(IV) Complexes

The work is focused on anticancer properties of dipicolinate (dipic)-based vanadium­(IV) complexes [VO­(dipic)­(N∩N)] bearing different diimines (2-(1H-imidazol-2-yl)­pyridine, 2-(2-pyridyl)­benzimidazole, 1,10-phenanthroline-5,6-dione, 1,10-phenanthroline, and 2,2′-bipyridine), as well as different...

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Published in:Journal of medicinal chemistry 2023-07, Vol.66 (13), p.8580-8599
Main Authors: Choroba, Katarzyna, Filipe, Beatriz, Świtlicka, Anna, Penkala, Mateusz, Machura, Barbara, Bieńko, Alina, Cordeiro, Sandra, Baptista, Pedro V., Fernandes, Alexandra R.
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents - pharmacology
Apoptosis
Cell Line, Tumor
Chick Embryo
Coordination Complexes - toxicity
Female
Humans
Ovarian Neoplasms
Phenanthrolines - pharmacology
Vanadium
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Summary:The work is focused on anticancer properties of dipicolinate (dipic)-based vanadium­(IV) complexes [VO­(dipic)­(N∩N)] bearing different diimines (2-(1H-imidazol-2-yl)­pyridine, 2-(2-pyridyl)­benzimidazole, 1,10-phenanthroline-5,6-dione, 1,10-phenanthroline, and 2,2′-bipyridine), as well as differently 4,7-substituted 1,10-phenanthrolines. The antiproliferative effect of V­(IV) systems was analyzed in different tumors (A2780, HCT116, and HCT116-DoxR) and normal (primary human dermal fibroblasts) cell lines, revealing a high cytotoxic effect of [VO­(dipic)­(N∩N)] with 4,7-dimethoxy-phen (5), 4,7-diphenyl-phen (6), and 1,10-phenanthroline (8) against HCT116-DoxR cells. The cytotoxicity differences between these complexes can be correlated with their different internalization by HCT116-DoxR cells. Worthy of note, these three complexes were found to (i) induce cell death through apoptosis and autophagy pathways, namely, through ROS production; (ii) not to be cytostatic; (iii) to interact with the BSA protein; (iv) do not promote tumor cell migration or a pro-angiogenic capability; (v) show a slight in vivo anti-angiogenic capability, and (vi) do not show in vivo toxicity in a chicken embryo.
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.3c00255