Synthesis and antiproliferative activity of quinolone nucleosides against the human myelogenous leukemia k-562 cell line.

摘要: A set of 6-substituted quinolone nucleosides linked to aniline or phenol via N O heteroatom-bridges presenting new compounds were synthesized by palladium-catalyzed Buchwald–Hartwig cross-coupling reactions. 6-Bromoquinolone nucleoside precursors, being protected either benzoyl TBDMS protecting groups on the ribose moiety, subjected different conditions as key step. Defined deprotection steps led, in good yields, final target that carry, position 3, ester, acid, amide functions. Thus, a series novel derivatives was obtained convergent synthesis route. Biological tests human chronic myelogenous leukemia K562 cells exerted an efficient antiproliferative activity for two them without induction differentiation. These deserve further experiments determine their effects other CML cell lines.