Synthesis, characterization and antitumor studies of N-aroyl-N'-thioaroylhydrazines and their Co(II), Ni(II), Cu(II) and Zn(II) complexes.
N-Salicyloyl-N'-p-hydroxythiobenzohydrazide (H2STPH) and N-benzoyl-N'-thiobenzohydrazide (H2BTBH) and their Co(II), Ni(II), Cu(II) and Zn(II) complexes were prepared and characterized by physicochemical studies. IR and NMR spectral studies imply dibasic tetradentate behaviour of the ligands bonding through 'thiolato' sulfur, enolic oxygen and the two hydrazinic nitrogens in a polymeric fashion. The electronic spectra indicate [Ni(STPH)(H2O)2], [Co(STPH)(H2O)2] to be distorted octahedral while [Cu(BTBH)] has a square-planar geometry. In vitro antitumor results of the ligand and the complexes on P-815 (murine mastocytoma) and L-929 (murine fibroblast) indicate that these compounds show significant inhibition of 3H-thymidine and 3H-uridine incorporation in DNA and RNA, respectively, in these tumor cells at dose levels of 1, 2.5 and 5 microg cm(-3). Antitumor studies suggest that [Cu(BTBH)] has significant dose dependent inhibitory effect on DNA synthesis. In vivo administration of [Cu(BTBH)] and [Ni(STPH)(H2O)2] resulted into prolongation of life span of Dalton's Lymphoma (DL) bearing mice.
Singh
Nand Kishore
NK
Department of Chemistry, Banaras Hindu University, Varanasi 221 005, India. nksingh@banaras.ernet.in
Singh
Saty Brat
SB
Singh
Nagendra
N
Shriviastav
Anuraag
A
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D003035:Cobalt / Q000737:chemistry; D003300:Copper / Q000737:chemistry; D006834:Hydrazines / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D019216:Metals, Heavy / Q000737:chemistry*; D051379:Mice; D009532:Nickel / Q000737:chemistry; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D012457:Salicylamides / Q000737:chemistry*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D013871:Thiones / Q000737:chemistry*; D014407:Tumor Cells, Cultured; D015032:Zinc / Q000737:chemistry
D000970:Antineoplastic Agents; D006834:Hydrazines; D008024:Ligands; D019216:Metals, Heavy; C478656:N-benzoyl-N'-thiobenzohydrazide; C105907:N-salicyloyl-N'-(4-hydroxybenzthioyl)hydrazine; D009942:Organometallic Compounds; D012457:Salicylamides; D013871:Thiones; D003035:Cobalt; D003300:Copper; D009532:Nickel; D015032:Zinc