Mixed-ligand copper(<scp>ii</scp>)-diimine complexes of 3-formylchromone-<i>N</i><sup>4</sup>-phenyl thiosemicarbazone: 5,6-dmp co-ligand confers enhanced cytotoxicity
Anjaneyulu Mamindla, Dhanashree Murugan, Manikandan Varadhan, Tamilarasan Ajaykamal, Loganathan Rangasamy, Mallayan Palaniandavar, Venugopal Rajendiran
Abstract
, 1.26 μM) against HeLa cervical cancer cells, and rendering it 5 times more potent than the widely used drug cisplatin. The same complex induces enhanced apoptotic cell death on HeLa cells but lower toxicity towards the non-cancerous PBMC cells. Molecular docking studies suggest that all the complexes bind in the minor groove of DNA and subdomain II of HSA, which is in close agreement with the experimental results. Also, 3 shows cytotoxicity higher than the analogous mixed ligand Cu(ii) complexes, reported already, emphasizing the importance of co-ligand in tuning the anticancer activity.
Topics & Concepts
DiimineCytotoxicityLipophilicityChemistryHeLaLigand (biochemistry)SemicarbazoneCopperDNARedoxCleaveApoptosisStereochemistryMedicinal chemistryIn vitroBiochemistryInorganic chemistryReceptorOrganic chemistryCatalysisMetal complexes synthesis and propertiesSynthesis and Characterization of Heterocyclic CompoundsSynthesis and biological activity