Synthesis, DNA/protein binding and in vitro cytotoxic studies of new palladium metallothiosemicarbazones

• Published in: Bioorganic & medicinal chemistry Vol. 21; no. 21; pp. 6742 - 6752
• Main Authors: Prabhakaran, R., Kalaivani, P., Poornima, P., Dallemer, F., Huang, R, Vijaya Padma, V., Natarajan, K.
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01-11-2013
• Subjects: Animals; binding capacity; BSA binding; Cattle; Cell Line, Tumor; Cell Survival - drug effects; Cellular uptake; chloroplast DNA; Coordination Complexes - chemical synthesis; Coordination Complexes - metabolism; Coordination Complexes - toxicity; Crystallography, X-Ray; CT-DNA binding; Cytotoxicity; DNA - chemistry; DNA - metabolism; Hep G2 Cells; Humans; Kinetics; liver neoplasms; lung neoplasms; Molecular Conformation; Nitrites - metabolism; palladium; Palladium - chemistry; Palladium(II) complexes; Protein Binding; Serum Albumin, Bovine - chemistry; Serum Albumin, Bovine - metabolism; Thiosemicarbazones; Thiosemicarbazones - chemistry; Cytotoxicity; Cellular uptake; BSA binding; Thiosemicarbazones; CT-DNA binding; Palladium(II) complexes
• ISSN: 0968-0896; 1464-3391
• DOI: 10.1016/j.bmc.2013.08.005

A series of four new thiosemicarbazone complexes of palladium have been synthesized, characterized and evaluated for their DNA/protein binding with CT-DNA and BSA, respectively. The new complexes bound to CT-DNA by intercalation mode and in protein binding studies, the complexes bound to BSA binding mechanism was found as static quenching. Among them the complex 4 had a strong binding affinity with BSA. In addition, in vitro cytotoxic studies were carried out on lung cancer (A549) and liver cancer (HepG2) cell lines and found that the complexes exhibited better activity than their parent thiosemicarbazone analogues. The complex 3 exhibited better activity than other complexes and this fact supported by the increased accumulation of the complexes in to the cancer cells which are evident from inter cellular uptake studies.