Aqueous dioxidovanadium(V)-aroylhydrazones: Role of biomolecular interactions, and hydrophobicity in anticancer potential

Abstract

Vanadium(V) complexes with aroylhydrazones having bio-important heterocyclic moieties in the ligand backbone are very efficient for cytotoxicity studies.1 Another important aspect for this class of compounds to be a good metallodrug is their solubility and stability in aqueous media which plays an important role in drug delivery to the targeted organ in its intact form. However, because of poor solubility many well-known therapeutic drugs found to be less effective with common side effects. Therefore, incorporating such moieties for synthesis of water soluble complexes could be fascinating for cytotoxicity studies. In this presentation, we have explored the detailed study on the synthesis and biological activity2,3 of some dioxidovanadium(V), [{VVO2L1–2}A(H2O)n]α (1−5), complexes with aroylhydrazone ligands having hetero cycles moiety incorporated with alkali metals (Na+, and K+) as counter cation.1 To study the biological behaviour, complexes were tested for solution phase stability, hydrophobicity, and DNA/BSA binding propensity experiments. Finally, the cytotoxicity study of 1−5 was performed against several cancer cell lines such as HeLa, HT- 29, MCF-7 and also for comparison a normal cell line NIH-3T3 was used. Remarkably, 1 with IC50 value = 5.42 ± 0.15 M showed greater activity than cisplatin against HT-29 cell line. However, in this study, we have established a relation of hydrophobic behavior of compounds directly to their anticancer activities. In addition, we found that 1−5 were selectively effective against HT-29 cells in comparison with MCF-7 and HeLa cells.