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

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, A2780<i>cis</i>, and OVCAR-3 human ovarian cancer cell lines. The dirhodium(I...

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Main Authors: Stephen de Doncker, Eva Fischer-Fodor, Cătălin Ioan Vlad, Patriciu Achimas-Cadariu, Gregory S. Smith, Siyabonga Ngubane
Format: Article
Language:English
Published: MDPI AG 2023-03-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/28/6/2671
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author Stephen de Doncker
Eva Fischer-Fodor
Cătălin Ioan Vlad
Patriciu Achimas-Cadariu
Gregory S. Smith
Siyabonga Ngubane
author_facet Stephen de Doncker
Eva Fischer-Fodor
Cătălin Ioan Vlad
Patriciu Achimas-Cadariu
Gregory S. Smith
Siyabonga Ngubane
author_sort Stephen de Doncker
collection DOAJ
description 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, A2780<i>cis</i>, 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 A2780<i>cis</i> 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 IC<sub>50</sub> value in the OVCAR-3 cell line in comparison with the dirhodium(II,II) tetraacetate.
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spelling doaj.art-05b34ca560ae4272abc499436813316f2023-11-17T12:53:34ZengMDPI AGMolecules1420-30492023-03-01286267110.3390/molecules28062671Cytotoxicity Evaluation of Unmodified Paddlewheel Dirhodium(II,II)-Acetate/-Formamidinate Complexes and Their Axially Modified Low-Valent MetallodendrimersStephen de Doncker0Eva Fischer-Fodor1Cătălin Ioan Vlad2Patriciu Achimas-Cadariu3Gregory S. Smith4Siyabonga Ngubane5Department of Chemistry, University of Cape Town, Rondebosch, Cape Town 7701, South AfricaTumour Biology Department, The Oncology Institute “Prof. Dr. Ion Chiricuţă”, 400015 Cluj-Napoca, RomaniaDepartment of Surgery, The Oncology Institute “Prof. Dr. Ion Chiricuţă”, 400015 Cluj-Napoca, RomaniaDepartment of Surgery, The Oncology Institute “Prof. Dr. Ion Chiricuţă”, 400015 Cluj-Napoca, RomaniaDepartment of Chemistry, University of Cape Town, Rondebosch, Cape Town 7701, South AfricaDepartment of Chemistry, University of Cape Town, Rondebosch, Cape Town 7701, South AfricaTwo 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, A2780<i>cis</i>, 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 A2780<i>cis</i> 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 IC<sub>50</sub> value in the OVCAR-3 cell line in comparison with the dirhodium(II,II) tetraacetate.https://www.mdpi.com/1420-3049/28/6/2671metallodrugdirhodium(II,II)formamidinecytotoxicitymetallodendrimers
spellingShingle Stephen de Doncker
Eva Fischer-Fodor
Cătălin Ioan Vlad
Patriciu Achimas-Cadariu
Gregory S. Smith
Siyabonga Ngubane
Cytotoxicity Evaluation of Unmodified Paddlewheel Dirhodium(II,II)-Acetate/-Formamidinate Complexes and Their Axially Modified Low-Valent Metallodendrimers
Molecules
metallodrug
dirhodium(II,II)
formamidine
cytotoxicity
metallodendrimers
title Cytotoxicity Evaluation of Unmodified Paddlewheel Dirhodium(II,II)-Acetate/-Formamidinate Complexes and Their Axially Modified Low-Valent Metallodendrimers
title_full Cytotoxicity Evaluation of Unmodified Paddlewheel Dirhodium(II,II)-Acetate/-Formamidinate Complexes and Their Axially Modified Low-Valent Metallodendrimers
title_fullStr Cytotoxicity Evaluation of Unmodified Paddlewheel Dirhodium(II,II)-Acetate/-Formamidinate Complexes and Their Axially Modified Low-Valent Metallodendrimers
title_full_unstemmed Cytotoxicity Evaluation of Unmodified Paddlewheel Dirhodium(II,II)-Acetate/-Formamidinate Complexes and Their Axially Modified Low-Valent Metallodendrimers
title_short Cytotoxicity Evaluation of Unmodified Paddlewheel Dirhodium(II,II)-Acetate/-Formamidinate Complexes and Their Axially Modified Low-Valent Metallodendrimers
title_sort cytotoxicity evaluation of unmodified paddlewheel dirhodium ii ii acetate formamidinate complexes and their axially modified low valent metallodendrimers
topic metallodrug
dirhodium(II,II)
formamidine
cytotoxicity
metallodendrimers
url https://www.mdpi.com/1420-3049/28/6/2671
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