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- W2952936919 abstract "The synthesis and biological evaluation of N-[4-(2-trans-[([2,6-diamino-4(3H)-oxopyrimidin-5-yl]methyl)thio]cyclobutyl)benzoyl]-L-glutamic acid (1) is reported. Compound 1 is a potent dihydrofolate reductase (DHFR) inhibitor (Kj = 12 nM) with excellent in vitro cell culture growth inhibition (L1210, IC50 = 29 nM). Protection experiments showed that the cell growth inhibitory activity was due to DHFR inhibition. The key step in the synthesis was the coupling of a cyclobutylmethylthiol with the 5-bromo-2,6-diamino-4-oxopyrimidine 8." @default.
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- W2952936919 date "1995-09-01" @default.
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- W2952936919 title "Synthesis and biological evaluation of -<i>n</i>[4-(2-<i>trans</i>-[([2,6-diamino-4(3<i>H</i>)-oxopyrimidin-5-yl]methyl)thio]cyclobutyl)benzoyl] -l-glutamic acid a novel 5-thiapyrimidinone inhibitor of dihydrofolate reductase" @default.
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- W2952936919 doi "https://doi.org/10.1002/jhet.5570320514" @default.
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