40372-03-0Relevant articles and documents
Oligomer conjugates of heteropentacyclic nucleosides
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Page/Page column 35; 36; 37, (2015/12/09)
The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer.
Synthesis and antitumor activity of ribavirin imidates. A new facile synthesis of ribavirin amidine (1-β-D-ribofuranosyl-1,2,4-triazole-3-carboxamidine hydrochloride)
Kini,Robins,Avery
, p. 1447 - 1449 (2007/10/02)
Methyl 1-β-D-ribofuranosyl-1,2,4-triazole-3-carboximidate (4) and ethyl 1-β-D-ribofuranosyl-1,2,4-triazole-3-carboximidate (6) were synthesized and tested for antitumor and antiviral activity. A new facile synthesis of 1-β-D-ribofuranosyl-1,2,4-triazole-3-carboxamidine hydrochloride (5), starting with imidate 4, was also developed. The imidates 4 and 6 differed greatly in solubility and dosing requirements. Even so, both compounds exhibited significant activity in vivo against murine leukemia L1210. Nontoxic dosing with 4 also significantly diminished Friend leukemia induced splenomegaly. In contrast, neither imidate was active in vitro.