| Literature DB >> 7837231 |
S Manfredini1, P G Baraldi, R Bazzanini, M Marangoni, D Simoni, J Balzarini, E De Clercq.
Abstract
It is well-known that the introduction of vinyl and ethynyl moieties into nucleosides is of crucial importance for cytostatic, antiviral, or other biological activities. In this study 6- and 8-vinyl-and -ethynyluridine and -adenosine were prepared by a general procedure involving the palladium-catalyzed cross-coupling of trimethylsilylacetylene or vinyltributyltin. The introduction of a vinyl group at C-6 of uridine or an ethynyl group at C-8 of adenosine resulted in nucleoside derivatives showing cytostatic activity against several murine and/or human tumor cell lines. Interestingly, 8-vinyladenosine had pronounced selective inhibitory effects on human (Molt/4F and MT-4) versus murine (L1210 and FM3A) tumor cell lines.Entities:
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Year: 1995 PMID： 7837231 DOI： 10.1021/jm00001a025
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446