Synthesis of novel pyrimidine apiothionucleosides and in vitro evaluation of their cytotoxicity

摘要: Abstract A series of novel pyrimidine d - and l -apiothionucleosides were synthesized from -arabinose, respectively, following a common versatile overall high-yielding scheme. The key-step was regio- stereo-selective Pummerer rearrangement reaction between nucleobase an appropriately functionalized thiosugar moiety. role the protecting group on side hydroxymethyl studied in terms productivity selectivity reactions involved synthetic Evaluation cytotoxic effects prepared compounds by MTT assay has shown that some them exhibit potent antitumor activity (IC50 3–20 μM) against specific cancer cell lines, whereas none had inhibitory effect normal line tested.