Seven-membered ring compounds as inhibitors of cytidine deaminase

摘要

Seven-membered heterocyclic nucleosides used to inhibit the deamination enzyme responsible for the inactivation of arabinosylcytosine (ara-C). Preferred nucleosides containing a seven-member aglycone are as follows: <IMAGE> R = H, benzoyl, para- nitrobenzoyl X = H, OR A = R, mono-, di- and tri- phosphates (PO3E2, P2O6E3, P3O9E4) E = H, Na Preferred aglycones are as follows: <IMAGE> 1a: X = OCH2CH2O 1b: X = SCH2CH2S 1c: X = O 1d: X = H, OH 1e: X = 2H Active components utilized against pyrimidine deaminases from mammalian tissues (mouse kidney and human liver) showed optimum advantage when compared with tetrahydrouridine (THU).