Structure–activity relationships of untenone A and its derivatives for inhibition of DNA polymerases

• Published in: Bioorganic & medicinal chemistry letters Vol. 14; no. 8; pp. 1975 - 1977
• Main Authors: Saito, Fumiyo, Takeuchi, Ryo, Kamino, Tomoyuki, Kuramochi, Kouji, Sugawara, Fumio, Sakaguchi, Kengo, Kobayashi, Susumu
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 19.04.2004; Elsevier
• Subjects: Antineoplastic agents; Biological and medical sciences; Cyclopentanes - chemical synthesis; Cyclopentanes - pharmacology; DNA Nucleotidylexotransferase - antagonists & inhibitors; Enzyme Inhibitors - chemical synthesis; Enzyme Inhibitors - pharmacology; Formates - chemical synthesis; Formates - pharmacology; General aspects; Humans; Indans - chemical synthesis; Indans - pharmacology; Levulinic Acids - chemical synthesis; Levulinic Acids - pharmacology; Medical sciences; Molecular Structure; Nucleic Acid Synthesis Inhibitors; Pharmacology. Drug treatments; Structure-Activity Relationship; Human; Diol; Enzyme; Transferases; Ketol; In vitro; Ester; Nucleotidyltransferases; Structure activity relation; Ketoester; Inhibition; Chemical synthesis; Enone; Monocyclic compound; DNA-directed DNA polymerase
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2004.01.092

We found that untenone A and mannzamenone A inhibit mammalian DNA polymerases α and β, and human terminal deoxynucleotidyl transferase (TdT). The syntheses of both compounds and the structure–activity relationships of untenone A derivatives are described. Graphic