European journal of medicinal chemistry, 35(5), 545-552 (2000-07-12)
4-hydroxy-2-pyridone derivatives 2 were prepared by reaction of 3-amino-3-dialkylaminopropenoates with bis(2,4, 6-trichlorophenyl)malonate. These compounds were further reacted with a set of aldehydes to give bis(pyridyl)methanes 3 and 4. The newly synthesized compounds 2, 3 and 4 were evaluated in vitro
One hundred and five nucleobase analogues were screened as inhibitors of dihydrouracil dehydrogenase (DHUDase, EC 1.3.1.2) from mouse liver. 5-Benzyloxybenzyluracil, 1-deazauracil (2,6-pyridinediol), 3-deazauracil (2,4-pyridinediol), 5-benzyluracil, 5-nitrobarbituric acid and 5,6-dioxyuracil (alloxan) were identified as potent inhibitors of this activity, with apparent
The breakdown of 5-fluoro-2'-deoxyuridine (FdUrd) to 5-fluorouracil (FUra) is catalyzed by the pyrimidine nucleoside phosphorylases, uridine phosphorylase and thymidine phosphorylase. The effects of nucleoside phosphorylase inhibitors on FdUrd and FUra elimination by the isolated perfused rat liver were investigated. The
New method for a synthesis of diazaphenoxathiin skeleton from 3-deazauracil derivatives is reported. It became possible to convert 3-deazauridine to 3-deazacytidine via an excellent intermediate "diazaphenoxathiin sulfoxide derivative".
European journal of medicinal chemistry, 38(1), 37-47 (2003-02-21)
Bis(pyridyl)methane derivatives 5-40 were obtained from the reaction of 4-hydroxy-2-pyridones 3 and 4 with aldehydes. Compounds 5-40 were evaluated for cytotoxic activity against a panel of 60 human cancer cell lines by the National Cancer Institute and some of them
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