engleski

Synthesis of Novel Aliphatic N-sulfonylamidino Thymine Derivatives by Cu(I)-catalyzed Three-component Coupling Reaction

A series of new aliphatic N-sulfonylamidino thymine derivatives containing nucleobase, N-sulfonyl and amidine pharmacophores in the structure were synthesized by Cu(I)-catalyzed three component coupling of 1-propargyl thymine, benzenesulfonyl azides and amines or ammonium salts. Preliminary in vitro antitumor screening (human cervix adenocarcinoma -HeLa and leukemia cells - Jurkat)revealed promising activities of N, N-diethyl- (2) and N-4-cyanobenzyl- (6) derivatives of 4-acetamidobenzenesulfonyl amidine.

alkynes; azides; copper; nucleobases; N-sulfonylamidine

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