Novel cytotoxic oxovanadium(IV) complexes: Influence of pyrazole-incorporated heterocyclic scaffolds on their biological response

作者：Gajera Sanjay B; Mehta Jugal V; Kanthecha Darshana N; Patel Ravi R; Patel Mohan N^*

来源：Applied Organometallic Chemistry, 2017, 31(11): e3767.

DOI：10.1002/aoc.3767

• antibacterial
• CT-DNA
• molecular docking
• oxovanadium(IV) complexes
• S. pombe

Homoleptic VOIV complexes with bidentate heterocycles, namely bipyrazole/pyrimidin-2-amine/triazolopyrimidine derivatives, are novel square pyramidal oxovanadium(IV) complexes. Their identities have been established using physicochemical techniques, namely elemental and spectral (ESI-MS, IR, UV-visible) analyses. The in vitro antibacterial activities against Gram-negative and Gram-positive microorganisms have been studied for all compounds, exhibiting good inhibition as compared to the ligands. In addition, all compounds exhibit significant cytotoxicity towards brine shrimp with LD50 values obtained in the range 8-24g ml(-1). Cellular level cytotoxicity has been investigated using bioassay of Schizosaccharomyces pombe, the complexes showing inevitable viability as concentration increases. Notably, UV absorption spectral titrations of the synthesized complexes with DNA reveal that the complexes bind to calf thymus DNA (CT-DNA) through intercalation mode (K-b=10(4)-10(5)M(-1)). Molecular docking reveals that the compounds are stacked between the base pairs of DNA. The results suggest that the complexes show promising binding affinity compared to the ligands towards CT-DNA.

• 出版日期2017-11