Cytotoxicity Evaluation of Unmodified Paddlewheel Dirhodium(II,II)-Acetate/-Formamidinate Complexes and Their Axially Modified Low-Valent Metallodendrimers

Eva Fischer-Fodor & Siyabonga Ngubane et al. · 2023-03-15

Two diphenyl formamidine ligands, four dirhodium(II,II) complexes, and three axially modified low-valent dirhodium(II,II) metallodendrimers were synthesized and evaluated as anticancer agents against the A2780, A2780cis, and OVCAR-3 human ovarian cancer cell lines. The dirhodium(II,II) complexes show moderate cytotoxic activity in the tested tumor cell lines, with acetate and methyl-substituted formamidinate compounds displaying increased cytotoxicity that is relative to cisplatin in the A2780cis cisplatin resistant cell line. Additionally, methyl- and fluoro-substituted formamidinate complexes showed comparable and increased cytotoxic activity in the OVCAR-3 cell line when compared to cisplatin. The low-valent metallodendrimers show some activity, but a general decrease in cytotoxicity was observed when compared to the precursor complexes in all but one case, which is where the more active acetate-derived metallodendrimer showed a lower IC50 value in the OVCAR-3 cell line in comparison with the dirhodium(II,II) tetraacetate.

Journal
Molecules
Funding
University of Cape Town (UCT) Grant PN-III-P4-ID-PCE-2021-1572University of Cape Town (UCT) Grant PNIII-P3-116University of Cape Town (UCT) Grant UID: 104023University of Cape Town (UCT) Grant UID: 11768Department of Science and Technology of South Africa Grant PN-III-P4-ID-PCE-2021-1572Department of Science and Technology of South Africa Grant PNIII-P3-116Department of Science and Technology of South Africa Grant UID: 104023Department of Science and Technology of South Africa Grant UID: 11768Romanian National Authority for Scientific Research and Innovation UEFISCDI project Grant PN-III-P4-ID-PCE-2021-1572Romanian National Authority for Scientific Research and Innovation UEFISCDI project Grant PNIII-P3-116Romanian National Authority for Scientific Research and Innovation UEFISCDI project Grant UID: 104023Romanian National Authority for Scientific Research and Innovation UEFISCDI project Grant UID: 11768Romanian-South African Bilateral Cooperation Grant PN-III-P4-ID-PCE-2021-1572Romanian-South African Bilateral Cooperation Grant PNIII-P3-116Romanian-South African Bilateral Cooperation Grant UID: 104023Romanian-South African Bilateral Cooperation Grant UID: 11768National Research Foundation of South Africa Grant PN-III-P4-ID-PCE-2021-1572National Research Foundation of South Africa Grant PNIII-P3-116National Research Foundation of South Africa Grant UID: 104023National Research Foundation of South Africa Grant UID: 11768UCT URC Open Access Journal Publication Fund Grant PN-III-P4-ID-PCE-2021-1572UCT URC Open Access Journal Publication Fund Grant PNIII-P3-116UCT URC Open Access Journal Publication Fund Grant UID: 104023UCT URC Open Access Journal Publication Fund Grant UID: 11768