Anticancer Activity Test Research Articles

Antitumor activity of polycyano-substituted carbo- and heterocycles prepared from 3-(2,2-dialkylhydrazino)-4-R-1,1,2,2-tetracyanocyclopentanes

Anticancer activity tests have been carried out at the National Cancer Institute (USA) on a series of polycyano-substituted carbo- and heterocyclic compounds synthesized from 3-(2,2-dialkylhydrazino)-4-R-1,1,2,2-tetracyanocyclopentanes. It is established that 1,1,2,2-tetracyano-substituted derivatives are the most active, showing a high activity comparable with that of reference drugs with respect to colon, ovarian, prostate, and renal cancer. The antitumor effect of the investigated compounds is explained by the presence of dialkylhydrazino- and 1,1,2,2-tetracyanoethyl moieties in their structures.

Synthesis and pharmacological activities of some mononuclear Ru(II) complexes

A series of mononuclear Ru(II) complexes of the type [Ru(M) 2(U)] 2+, where M=2,2′-bipyridine/1,10-phenanthroline and U=tpl (Ru1), 4-Cl-tpl (Ru2), 4-CH 3-tpl (Ru3), 4-CH 3O-tpl (Ru4), and 4-NO 2-tpl (Ru5), -pai (Ru6), where tpl = thiopicolinanilide and pai = 2-phenyl-azo-imidazole, have been prepared and characterized by IR, UV–Vis, 1H NMR, 13C-NMR, FAB-Mass spectrophotometer, and elemental analysis. The complexes display metal–ligand charge transfer (MLCT) transitions in the visible region. The title complexes were subjected to in vivo anticancer activity tests against a transplantable murine tumor cell line, Ehrlich’s ascitic carcinoma (EAC) and in vitro antibacterial activity against Gram positive and Gram negative microorganisms. Ru1–Ru6 were found to increase the life span of the tumor hosts by 19–52%, and decreased tumor volume and viable ascitic cell count. The results of the present study clearly demonstrated the tumor inhibitory activity of the ruthenium chelates against transplantable murine tumor cell line. The treatment with ruthenium complexes could be secondary to tumor regression or due to the action of the compounds itself. The significant antibacterial activity was observed for Ru1–Ru4 against microorganisms like Vibrio cholera 865, Staphylococcus aureus 6571, and Shigella flexneri as compared to that of standard drug chloramphenical. Ru5 showed moderate activity against S. aureus 8530. However, all the complexes fail to show significant antibacterial activity against V. cholera 14033 and Shigella sonnai.

Synthesis of a series of vicinal diamines with potential biological activity

Abstract A broad range of vicinal diamines based on styrene oxide are synthesisedvia mixtures of regioisomeric amino alcohols. The ring opening of the intermediate aziridinium ions by primary amines proceeds with high regioselectivity, leading to the target diamines as single regioisomers for all reaction series. The compounds are of potential biological interest as ligands for cisplatin analogues. Anticancer activity tests of both groups of compounds are in progress.

Antineoplastic and Antibacterial Activity of some Mononuclear Ru(II) Complexes

These ligands (L) show a bidentate behavior, forming octahedral ruthenium complexes. The title complexes were subjected to in-vivo anticancer activity tests against a transplantable murine tumor cell line, Ehrlich's Ascitic Carcinoma (EAC) and in-vitro antibacterial activity against several Gram positive and Gram negative bacterial strains. [Ru(bpy)2(ihqs)]Cl2 and [Ru(bpy)2(hc)]Cl2 (where bpy=2,2′-bipyridine, ihqs=7-iodo-8hydroxy quinoline-5-sulphonic acid and hc=3-hydroxy coumarin) showed promising antitumor activity. Treatment with these complexes prolonged the life span of EAC bearing mice as well as decreased their tumor volume and viable ascitic cell count. All the tested complexes exhibited mild to moderate antibacterial activity.