engleski

Synthesis and Antitumor Activity of N-Sulfonyl Derivatives and Sulfonamido Nucleoside Derivatives

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.

synthesis; antitumor activity; N-sulfonyl derivatives; sulfonamido derivatives; nucleobase; nucleosides

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