The solid phase synthesis of tetrahydroisoquinolines having cdc25B inhibitory activity

E L Fritzen; A S Brightwell; L A Erickson; D L Romero

doi:10.1016/s0960-894x(00)00069-x

The solid phase synthesis of tetrahydroisoquinolines having cdc25B inhibitory activity

Bioorg Med Chem Lett. 2000 Apr 3;10(7):649-52. doi: 10.1016/s0960-894x(00)00069-x.

Authors

E L Fritzen¹, A S Brightwell, L A Erickson, D L Romero

Affiliation

¹ Medicinal Chemistry Research, Pharmacia & Upjohn Company, Kalamazoo, MI, 49001, USA. [email protected]

PMID: 10762045
DOI: 10.1016/s0960-894x(00)00069-x

Abstract

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.

MeSH terms

Cell Cycle Proteins / antagonists & inhibitors*
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology
Inhibitory Concentration 50
Isoquinolines / chemical synthesis*
Isoquinolines / chemistry
Isoquinolines / pharmacology
Structure-Activity Relationship
cdc25 Phosphatases / antagonists & inhibitors*

Substances

Cell Cycle Proteins
Enzyme Inhibitors
Isoquinolines
PNU 108937
cdc25 Phosphatases