The solid phase synthesis of tetrahydroisoquinolines having cdc25B inhibitory activity.
A solid phase synthesis of substituted tetrahydroisoquinolines was developed and used to prepare directed libraries of compounds for screening against the protein phosphatase, CDC25B. From these libraries, a compound was found having approximately a 4-fold improvement in activity.
Fritzen
E L
EL
Medicinal Chemistry Research, Pharmacia & Upjohn Company, Kalamazoo, MI, 49001, USA. edward.1.fritzen@am.pnu.com
Brightwell
A S
AS
Erickson
L A
LA
Romero
D L
DL
D018797:Cell Cycle Proteins / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D020687:cdc25 Phosphatases / Q000037:antagonists & inhibitors*
D018797:Cell Cycle Proteins; D004791:Enzyme Inhibitors; D007546:Isoquinolines; C412030:PNU 108937; D020687:cdc25 Phosphatases