SYNTHESIS AND BIOLOGICAL-ACTIVITY OF 5-SUBSTITUTED ANTI-CONSTRAINED ACYCLIC ANALOGS OF CYTIDINE AND URIDINE

A number of 5-substituted constrained acyclic analogs of cytidine and uridine have been prepared in which the glycosyl torsion angle is cons trained in the anti conformation. Compounds 2a-c, 3a-c, 4, 5 and 6 wer e tested for activity against HCMV and HSV-1. Compounds 2a and 2b show ed moderate activity against HCMV. Compound 2c exhibited a weak inhibi tory activity against HSV-1. Compounds 2a, 3a,4, 5, 6, 8, and 9 were s creened for their anti-HIV or antitumor activity. None of them were ac tive against HIV. However, compound 9 showed a 50% inhibition on MDA-M B-231/ATTC breast cancer cell growth at a concentration of 0.15 mu M.