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

Fumiyo Saito; Ryo Takeuchi; Tomoyuki Kamino; Kouji Kuramochi; Fumio Sugawara; Kengo Sakaguchi; Susumu Kobayashi

doi:10.1016/j.bmcl.2004.01.092

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

Bioorg Med Chem Lett. 2004 Apr 19;14(8):1975-7. doi: 10.1016/j.bmcl.2004.01.092.

Authors

Fumiyo Saito¹, Ryo Takeuchi, Tomoyuki Kamino, Kouji Kuramochi, Fumio Sugawara, Kengo Sakaguchi, Susumu Kobayashi

Affiliation

¹ Frontier Research Center for Genome and Drug Discovery, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan.

PMID: 15050640
DOI: 10.1016/j.bmcl.2004.01.092

Abstract

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

MeSH terms

Cyclopentanes / chemical synthesis
Cyclopentanes / pharmacology*
DNA Nucleotidylexotransferase / antagonists & inhibitors
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / pharmacology
Formates / chemical synthesis
Formates / pharmacology*
Humans
Indans / chemical synthesis
Indans / pharmacology*
Levulinic Acids / chemical synthesis
Levulinic Acids / pharmacology*
Molecular Structure
Nucleic Acid Synthesis Inhibitors*
Structure-Activity Relationship

Substances

Cyclopentanes
Enzyme Inhibitors
Formates
Indans
Levulinic Acids
Nucleic Acid Synthesis Inhibitors
manzamenone A
plakevulin A
untenone A
DNA Nucleotidylexotransferase