hrvatski

Derivati purinskih bioizostera i pirimidina s 1, 2, 3- triazolom kao farmakoforom

Introduction of a 1, 2, 3-triazole ring into nucleosides to improve their bioactivity for antitumor or antiviral applications has become wide spread. The click chemistry reactions of nucleosides and nucleotides have found wide application in lead identification and lead optimization procedures in drug design. The 1, 2, 3- triazole unit may be considered as a surrogate of the amide group because it has H-bond acceptor capacity, distance between substituents and dipolar properties similar to the peptide bond. Keeping into consideration the biological potency of 1, 2, 3-triazolo-nucleosides [1, 2] and in our continuous endeavor toward the synthesis of pharmacologically active molecules, we designed the synthesized 1, 2, 3-triazole embedded N- heterocycles in order to evalute their cytostatic activities. The target regioselective 1, 4- disubstituted 1, 2, 3-triazole derivatives were prepared by the Cu-catalyzed alkyne-azide cycloaddition (CuAAC). Linear alkyl chain, substituted aromatic moiety and cyclopropyl ring were introduced as alkynyl substituents at C-5 and N-3 of pyrimidine core using palladium catalysed cross-coupling Sonogashira reaction. Evaluations of cytostatic activities of the synthesyzed compounds are currently underway.

1 ; 2 ; 3-triazoli ; purinski bioizosteri ; cikloadicija alkina i azida ; citostatska djelovanja

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