Inhibitors of Dihydrofolate Reductase, 8-Oxapteridines

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The biological activities of some homeosterically related analogs of dihydrofolic acid have been examined involving pyrimido[4,5-b][l,4]oxazine (8-oxapteridine) derivatives. It is anticipated that these compounds might interfere with the essential intermediary metabolic functions of the vitamin and thus serve as potential chemotherapeutic agents. Preliminary toxicity studies in microbial assay systems were disappointing; however, inhibitory effects were demonstrated in cell free enzyme systems. A comparison of the structure/activity relationships was determined using two folic acid coenzyme systems, dihydrofolate reductase and thymidylate synthetase. The 2-amino-4-hydroxy-6-(substituted)-8-oxapteridines were generally more effective inhibitors than the corresponding 2,4-diamino analogs. The relative biological activity of a series of ... continued below

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v, 42 leaves : illustrations

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Lin, Shwu-Ching H. December 1974.

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  • Lin, Shwu-Ching H.

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The biological activities of some homeosterically related analogs of dihydrofolic acid have been examined involving pyrimido[4,5-b][l,4]oxazine (8-oxapteridine) derivatives. It is anticipated that these compounds might interfere with the essential intermediary metabolic functions of the vitamin and thus serve as potential chemotherapeutic agents.
Preliminary toxicity studies in microbial assay systems were disappointing; however, inhibitory effects were demonstrated in cell free enzyme systems. A comparison of the structure/activity relationships was determined using two folic acid coenzyme systems, dihydrofolate reductase and thymidylate synthetase.
The 2-amino-4-hydroxy-6-(substituted)-8-oxapteridines were generally more effective inhibitors than the corresponding 2,4-diamino analogs. The relative biological activity of a series of 2-amino-4-hydroxy-6-ω-phenylalkyl derivatives were examined, and the most active derivative was the 6-phenylethyl analog which appears to function as a mixed-type inhibitor involving partially competitive and partially non-competitive inhibition.

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v, 42 leaves : illustrations

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UNT Theses and Dissertations

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  • December 1974

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  • June 24, 2015, 9:39 a.m.

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  • Sept. 15, 2016, 8:33 p.m.

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Lin, Shwu-Ching H. Inhibitors of Dihydrofolate Reductase, 8-Oxapteridines, thesis, December 1974; Denton, Texas. (digital.library.unt.edu/ark:/67531/metadc663439/: accessed July 23, 2018), University of North Texas Libraries, Digital Library, digital.library.unt.edu; .