engleski

Synthesis, Structural Characterisation and Biological Activity of Zn(II) and Pd(II) Complexes of 3-Substituted 5-(2'-Pyridyl)- 1, 4-benzodiazepin-2-one Derivatives

ZnII and PdII complexes of 7-bromo-1, 3-dihydro-3-hydroxymethyl-1-methyl-5-(2’-pyridyl)-2H-1, 4-benzodiazepin-2-one, (+)-L1, and 3-acetoxymethyl-7-bromo-1, 3-dihydro-1-methyl-5-(2’-pyridyl)-2H-1, 4-benzodiazepin-2-one, (ą)-L2 were prepared and determined by spectroscopic studies (IR and 1H NMR) and X-ray structure analysis. The influence of the metal coordination on the absolute configuration at the stereogenic centre of the chiral ligands was studied. In ZnL1Cl2 (1) a distorted trigonal bipyramide was formed in which L1 acts as a tridentate N, N, O-ligand, while in the case of ZnL2Cl2 (3), ZnII is in a distorted tetrahedral environment coordinated by two azomethine nitrogen and two chlorine atoms. ZnII complexes 1 and 3 are the first zinc complexes of benzodiazepines reported so far. In PdII complexes 2 and 4, the expected square-planar coordination was observed. The free ligands and their complexes were evaluated for their in vitro cytostatic activity against the murine L1210/0 and human T-lymphoblast Molt/C8 and CEM/0 cell lines, as well as for their in vitro antiviral activity in different assay systems.

chiral benzodiazepine ligands; zinc complexes; palladium complexes; spectroscopy; X-ray structure analysis; cytostatic and antiviral activity

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