Synthesis of a novel class of cdc25A inhibitors from vitamin D3.
We have developed a novel class of cdc25A inhibitors by drastic modification of the hydrophobic and hydrophilic substructures of dysidiolide. The unsaturated derivative 3b strongly inhibited cdc25A (IC50 = 7.7 microM) and caused GI arrest of HL60 cells.
Dodo
K
K
Institute of Molecular and Cellular Biosciences, The University of Tokyo, Japan.
Takahashi
M
M
Yamada
Y
Y
Sugimoto
Y
Y
Hashimoto
Y
Y
Shirai
R
R
D015107:4-Butyrolactone / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002762:Cholecalciferol / Q000031:analogs & derivatives* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016193:G1 Phase / Q000187:drug effects*; D018922:HL-60 Cells; D006801:Humans; D020687:cdc25 Phosphatases / Q000037:antagonists & inhibitors*
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D002762:Cholecalciferol; C517004:CDC25A protein, human; D020687:cdc25 Phosphatases; C121906:dysidiolide; D015107:4-Butyrolactone