Synthesis and biological evaluation of -n[4-(2-trans-[([2,6-diamino-4(3H)-oxopyrimidin-5-yl]methyl)thio]cyclobutyl)benzoyl] -l-glutamic acid a novel 5-thiapyrimidinone inhibitor of dihydrofolate reductase
โ Scribed by Michael D. Varney; William H. Romines II; Theodore Boritzki; Stephen A. Margosiak; Charlotte Bartlett; Eleanor J. Howland
- Book ID
- 112131357
- Publisher
- Journal of Heterocyclic Chemistry
- Year
- 1995
- Tongue
- English
- Weight
- 526 KB
- Volume
- 32
- Category
- Article
- ISSN
- 0022-152X
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๐ SIMILAR VOLUMES
Nine novel nonclassical 2,4-diamino-6-methyl-5-thioarylsubstituted-7H-pyrrolo [2,3-d]pyrimidines 2-10 were synthesized as potential inhibitors of dihydrofolate reductase and as antitumor agents. The analogues contain various electron donating and electron withdrawing substituents on the phenylsulfan
A novel series of dihydrofolate reductase inhibitors was uncovered during an expansion of the SAR of 5,10-dideazatetrahydrofolic acid, and their biological activity was evaluated. These new analogs do not possess an oxygen at the 4 position and contain a monocyclic pyrimidine ring.