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Differential transmetallation of complexes of the anti-cancer thiosemicarbazone, Dp4e4mT: effects on anti-proliferative efficacy, redox activity, oxy-myoglobin and oxy-hemoglobin oxidation

Mahendiran Dharmasivam, Büşra Kaya, Tharushi P. Wijesinghe, Věra Richardson, Jeffrey R. Harmer, Miguel A. Gonzálvez, William Lewis, Mahan Gholam Azad, Paul V. Bernhardt, Des R. Richardson

2023Chemical Science21 citationsDOIOpen Access PDF

Abstract

: 0.262-1.570 μM after 72 h), probably due to a lack of transmetallation with Cu(ii). The poor efficacy of the Dp4e4mT Co(iii), Ni(ii), and Pd(ii) complexes to transmetallate with Fe(iii) markedly suppresses the oxidation of oxy-Mb and oxy-Hb. In contrast, the 2 : 1 Dp4e4mT: Cu(ii), Zn(ii), and Ga(iii) complexes demonstrate facile reactions with Fe(iii), leading to the redox active Dp4e4mT Fe(iii) complex and oxy-Mb and oxy-Hb oxidation. This study demonstrates the key role of differential transmetallation of Dp4e4mT complexes that has therapeutic ramifications for their use as anti-cancer agents.

Topics & Concepts

TransmetalationChemistryHemoglobinSemicarbazoneMyoglobinRedoxMedicinal chemistryStereochemistryNuclear chemistryBiochemistryCatalysisInorganic chemistryMetal complexes synthesis and propertiesTrace Elements in HealthRadiopharmaceutical Chemistry and Applications
Differential transmetallation of complexes of the anti-cancer thiosemicarbazone, Dp4e4mT: effects on anti-proliferative efficacy, redox activity, oxy-myoglobin and oxy-hemoglobin oxidation | Litcius