Synthesis and biological evaluation of N-[4-(2-trans-[([2,6-diamino-4(3H)-oxopyrimidin-5-yl]methyl)thio]cyclo butyl)benzoyl]-L-glutamic acid a novel 5-thiepyrimidinone inhibitor of dihydrofolate reductase

DOI: 10.1002/jhet.5570320514

Source and publish data:

Journal of Heterocyclic Chemistry p. 1493 - 1498 (1995)

Update date:2022-09-26

Topics:

Authors:

Varney Varney

Romines III

Boritzki

Margosiak

Bartlett

Howland Howland

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Article abstract of DOI:10.1002/jhet.5570320514

The synthesis and biological evaluation of N-[4-(2-trans-[([2,6-diamino-4(3H)-oxopyrimidin-5-yl]methyl)thio]cyclo butyl)benzoyl]-L-glutamic acid (1) is reported. Compound 1 is a potent dihydrofolate reductase (DHFR) inhibitor (K(i) = 12 nM) with excellent

Full text of DOI:10.1002/jhet.5570320514

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