Design and synthesis of novel Cdc25A-inhibitors having phosphate group as a hydrophilic residue.
Compounds (6a-e) were synthesized by phosphorylation of hydrophobic perhydroindan derivatives derived from vitamin D(3), and were found to show strong inhibitory activity towards dual-specificity phosphatase Cdc25A (IC(50)=0.7-24.5 microM).
Shimazawa
Rumiko
R
Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
Gochomori
Mika
M
Shirai
Ryuichi
R
D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D010710:Phosphates / Q000737:chemistry*; D020687:cdc25 Phosphatases / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D010710:Phosphates; D020687:cdc25 Phosphatases