DNA polymerase beta inhibitors from Sandoricum koetjape.
Bioassay-guided fractionation of Sandoricum koetjape using an assay sensitive to DNA polymerase beta inhibition led to the isolation of three active compounds (1-3) having IC(50) values from 20 to 36 microM. Derivatives 5-14 were prepared from compounds 1 and 2; derivatives 11, 12, and 13 showed activity against DNA polymerase beta with IC(50) values ranging from 16 to 36 microM.
Sun
D A
DA
Departments of Chemistry and Biology, University of Virginia Charlottesville, Virginia 22901, USA.
Starck
S R
SR
Locke
E P
EP
Hecht
S M
SM
D019951:DNA Polymerase beta / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000302:isolation & purification* / Q000494:pharmacology; D007700:Kinetics; D019441:Plant Epidermis / Q000737:chemistry; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D010946:Plants, Medicinal / Q000737:chemistry*; D014934:Wood
D004791:Enzyme Inhibitors; D010936:Plant Extracts; D019951:DNA Polymerase beta