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We have designed and synthesized N-sulfonyl derivatives of pyrimidine bases as a new type of sulfonylcycloureas. These type of compounds showed potent growth inhibitory activity against human tumor cell lines in vitro, at concentrations of 10-8− 10-5 M (25-75%), and some of them showed the ability to induce apoptosis in treated tumor cells. These results directed our interest toward N-sulfonyl derivatives of purine bases and sulfonamido derivatives of nucleosides. The synthesis involves the reaction of purine base or amino function of modified purine nucleoside with sulfonyl chlorides in pyridine. The introduction of the sulfonamido group on the C-2 position of the pyrimidine nucleosides was achieved by ring opening of 2, 3’ - and 2, 2’ -anhydronucleosides with appropriate sulfonamide anion as nucleophile. The synthesis and antitumor activity of the target nucleoside derivatives will be presented.

Spectroscopic ( 1 H NMR, UV-visible) and biological (cytostatic, antiviral activity) studies of palladium(II) complexes of monoethyl 2-quinolymethylphosphonate (2-Hmqmp): dihalide adducts trans -Pd(2-Hmqmp) 2 X 2 , chelate Pd(2-mqmp) 2 · 2H 2 O and ion-pair salt complexes [2-H 2 mqmp] + [Pd(2-Hmqmp)X 3 ] − (X=Cl, Br), have been carried out in order to determine structural and biological properties of these biologically interesting complex compounds. The complexes were evaluated in vitro for their cytostatic activity against murine L1210 and human KB and T-lymphoblast Molt4/C8 and CEM/0 cell lines, and the results obtained were compared with those obtained for the complexes of diethyl 2-quinolylmethylphosphonate (2-dqmp). The L1210 cell was the most responsive line and complexes of diester 2-dqmp were more active than complexes of monoester 2-Hmqmp. A good relationship was observed between the cytostatic activity of the complexes and their lypophilicity or solubility. Some complexes exhibited significant cell growth inhibitory effects, but none of the them was more cytostatic than cisplatin. Both 2-dqmp and 2-Hmqmp complexes were also evaluated in vitro for their antiviral activity in different assay systems, comprising a broad spectrum of DNA and RNA viruses, but no specific antiviral effects were noted. In addition, the complexes did not show any specific anti-HIV activity.