Synthesis and Cytostatic Activity of Novel 6-(Difluoromethyl)purine Bases and Nucleosides

Abstract

An expeditious synthesis of modified purine bases and nucleosides bearing a difluoromethyl group in position 6 is described starting from the corresponding 6-(hydroxymethyl)purine derivatives. Their oxidation using Dess-Martin reagent gave 6-formylpurines that were converted to the title compounds by reaction with Deoxofluor. 6-(Difluoromethyl)purine ribonucleoside exerted significant cytostatic effect against leukemia cell lines.

Key words

purines - nucleobases - nucleosides - fluorination - anti­neoplastic activity

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