Choroba, KatarzynaFilipe, BeatrizŚwitlicka, AnnaPenkala, MateuszMachura, BarbaraBieńko, AlinaCordeiro, SandraBaptista, Pedro V.Fernandes, Alexandra R.2023-11-202023-11-202023-07-130022-2623PURE: 75590433PURE UUID: c29e8b46-720b-4d9c-885b-e7368d55fad3Scopus: 85163606203WOS: 001008566000001PubMed: 37311060PubMedCentral: PMC10350923ORCID: /0000-0001-5255-7095/work/151383883ORCID: /0000-0003-2054-4438/work/151392211http://hdl.handle.net/10362/160196funds granted under the Research Excellence Initiative of the University of Silesia in Katowice. The authors thank Dr inż. Mariola Siwy for measurements of elemental analysis. Publisher Copyright: © 2023 The Authors. Published by American Chemical Society.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.205240679engMolecular MedicineDrug DiscoverySDG 3 - Good Health and Well-beingjournal article10.1021/acs.jmedchem.3c00255https://www.scopus.com/pages/publications/85163606203