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

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

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2004-04, Vol.14 (8), p.1975-1977
Hauptverfasser:	Saito, Fumiyo, Takeuchi, Ryo, Kamino, Tomoyuki, Kuramochi, Kouji, Sugawara, Fumio, Sakaguchi, Kengo, Kobayashi, Susumu
Format:	Artikel
Sprache:	eng
Schlagworte:	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
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Beschreibung
Zusammenfassung:	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
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2004.01.092