SYNTHESIS AND BIOLOGICAL ACTIVITY OF 5-SUBSTITUTED ANTI-CONSTRAINED ACYCLIC ANALOGS OF CYTIDINE AND URIDINE |
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| Authors: | Ling-Yih Hsu Ya-Mei Chang Chung-Hsun Lin John C Drach |
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| Institution: | 1. School of Pharmacy , National Defense Medical Center , Taipei, Republic of China;2. Deparment of Biologic and Materials Sciences School of Dentistry , University of Michigan , Ann Arbor, Michigan, 48109-1078, USA |
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| Abstract: | Abstract Abstract. A number of 5-substituted constrained acyclic analogs of cytidine and uridine have been prepared in which the glycosyl torsion angle is constrained in the anti conformation. Compounds 2a-c, 3a-c, 4, 5 and 6 were tested for activity against HCMV and HSV-1. Compounds 2a and 2b showed moderate activity against HCMV. Compound 2c exhibited a weak inhibitory activity against HSV-1. Compounds 2a, 3a, 4, 5, 6, 8, and 9 were screened for their anti-HIV or antitumor activity. None of them were active against HIV. However, compound 9 showed a 50% inhibition on MDA-MB-231/ATTC breast cancer cell growth at a concentration of 0.15 μM. |
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