Bioactivities of simplified adociaquinone B and naphthoquinone derivatives against Cdc25B, MKP-1, and MKP-3 phosphatases.
Some simplified adociaquinone B analogs and a series of 1,4-naphthoquinone derivatives were synthesized and tested against the three enzymes Cdc25B, MKP-1, and MKP-3. Cdc25B and MKP-1 in particular are enzymes overexpressed in human cancer cells, and they represent potential molecular targets for novel cancer chemotherapeutic treatments. A number of analogs exhibited significant inhibitory activity against these enzymes, and the bioassay data in addition to structure-activity relationships of these compounds will be discussed.
Cao
Shugeng
S
Department of Chemistry, Virginia Polytechnic Institute and State University, 3111 Hahn Hall, M/C 0212, Blacksburg, VA 24061, USA.
Murphy
Brian T
BT
Foster
Caleb
C
Lazo
John S
JS
Kingston
David G I
DG
D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003499:Cyclic S-Oxides / Q000494:pharmacology*; D054638:Dual Specificity Phosphatase 1 / Q000037:antagonists & inhibitors*; D054642:Dual Specificity Phosphatase 6 / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D009285:Naphthoquinones / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization; D020687:cdc25 Phosphatases / Q000037:antagonists & inhibitors*
D003499:Cyclic S-Oxides; D004791:Enzyme Inhibitors; D009285:Naphthoquinones; C541046:adociaquinone B; D054638:Dual Specificity Phosphatase 1; D054642:Dual Specificity Phosphatase 6; D020687:cdc25 Phosphatases