Critical structural motif for the catalytic inhibition of human topoisomerase II by UK-1 and analogs.
Three new analogs of UK-1 have been synthesized and their efficacies as topoisomerase II inhibitors have been determined. Results show that UK-1 and two of these analogs are catalytic inhibitors of topo II and identifies a critical structure motif necessary for enzyme inhibition.
Wang
Ben B
BB
Department of Chemistry and Biochemistry, University of Maryland, Baltimore County, Baltimore, MD 21250, USA.
Maghami
Nima
N
Goodlin
Vanessa L
VL
Smith
Paul J
PJ
D001583:Benzoxazoles / Q000737:chemistry* / Q000494:pharmacology; D002384:Catalysis / Q000187:drug effects; D004250:DNA Topoisomerases, Type II / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D018922:HL-60 Cells; D006801:Humans; D059005:Topoisomerase II Inhibitors
D001583:Benzoxazoles; D004791:Enzyme Inhibitors; D059005:Topoisomerase II Inhibitors; C082787:UK 1; D004250:DNA Topoisomerases, Type II