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Synthesis and cytostatic activity of 7-arylsulfanyl-7-deazapurine bases and ribonucleosides

Publikace na Přírodovědecká fakulta |
2015

Tento text není v aktuálním jazyce dostupný. Zobrazuje se verze "en".Abstrakt

A series of 7-phenylsulfanyl- or 7-(2-thienyl) sulfanyl-7-deazapurine bases bearing diverse substituents at position 6 was prepared through C-H sulfenylation of 6-chloro-7-deazapurine followed by cross-coupling or nucleophilic substitutions. The corresponding ribonucleosides (as thia-analogues of known nucleoside cytostatics) were prepared by glycosylation of 6-chloro-7-arylsulfanyl-7-deazapurines followed by the same transformations at position 6.

The 7-thienylsulfanyl-7-deazapurine bases 2b-2h exerted micromolar cytostatic activities, whereas the nucleosides did not show significant biological effects.