Protein Structure-Based Design, Synthesis, and Biological Evaluation of 5-Thia-2,6-diamino-4(3H)-oxopyrimidines: Potent Inhibitors of Glycinamide Ribonucleotide Transformylase with Potent Cell Growth Inhibition

The design, synthesis, biochemical, and biological evaluation of a novel series of 5-thia-2,6-diamino-4(3H)-oxopyrimidine inhibitors of glycinamide ribonucleotide transformylase (GART) are described. The compounds were designed using the X-ray crystal structure of human GART. The monocyclic 5-thiapy...

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Veröffentlicht in:	Journal of medicinal chemistry 1997-08, Vol.40 (16), p.2502-2524
Hauptverfasser:	Varney, Michael D, Palmer, Cindy L, Romines, William H, Boritzki, Theodore, Margosiak, Stephen A, Almassy, Robert, Janson, Cheryl A, Bartlett, Charlotte, Howland, Eleanor J, Ferre, Rosanne
Format:	Artikel
Sprache:	eng
Schlagworte:	Acyltransferases - antagonists & inhibitors Animals Antineoplastic agents Antineoplastic Agents - chemical synthesis Biological and medical sciences Cell Division - drug effects Crystallography, X-Ray Drug Design Escherichia coli Folic Acid - analogs & derivatives Folic Acid - metabolism General aspects Humans Hydroxymethyl and Formyl Transferases Medical sciences Mice Models, Molecular Pharmacology. Drug treatments Phosphoribosylaminoimidazolecarboxamide Formyltransferase Phosphoribosylglycinamide Formyltransferase Protein Conformation Pyrimidines - chemical synthesis Pyrimidines - chemistry Recombinant Proteins - antagonists & inhibitors Stereoisomerism Tumor Cells, Cultured
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