Synthesis and characterization of potential antitumour and antiviral gallium(III) complexes of N-heterocycles

摘要: Abstract Ten water-soluble gallium(III) complexes of N-heterocycles were synthesized and characterized by elemental analysis, conductivity measurements, IR spectroscopy, 1H NMR spectroscopy optical activity measurements. Raman spectra measured with two an X-ray singe-crystal study performed one complex—trans-dichlorotetrakis-(5-methylpyrazole)gallium(III)tetrachlorogallate(III). The had the general formulae: [L4GaCl2]GaCl4 (L = ligand) indazole, 1,2,3-benzotriazole, pyrazole, 5-methylpyrazole, 4-methylpyrazole), having a trans-octahedral structure (symmetry Ci), [L4GaCl2]Cl imidazole, benzimidazole), also configuration, LGaCl2 2-α-oxybenzylbenzimidazolato (HBB) respective enantiomers d (−)-HBB l (+)-HBB) tetrahedral structure. So far, eight have been tested in vitro anti-HIV test (HIV human immunodeficiency virus) National Cancer Institute (NCI) U.S.A., four these found to be moderately active: trans-dichlorotetrakis-(5-methylpyrazole)gallium(III) tetrachlorogallate(III), trans-dichlorotetrakis-(4-methylpyrazole)gallium(III)tetrachlorogallate(III), dichloro-(2-α-oxybenzylbenzimidazolato-N,O) gallium (III) trans-dichlorotetrakis(benzimidazole)gallium(III) chloride, latter exhibiting highest therapeutic index (TI) 77. For comparison, for 3′-azido-3′-deoxythymidine (AZT) ranges from TI 1000 4000.