Pyrazolo[4,3-d]pyrimidines as new generation of cyclin-dependent kinase inhibitors

Bioorg Med Chem Lett. 2003 Sep 15;13(18):2989-92. doi: 10.1016/s0960-894x(03)00631-0.

Abstract

A search among analogues of anti-CDK purines led to the identification of substituted pyrazolo[4,3-d]pyrimidines as novel inhibitors of CDK1/cyclin B. Some of these derivatives also show antiproliferative activity on cancer cell line K-562, thus may find an application as anticancer agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • CDC2 Protein Kinase / antagonists & inhibitors
  • Cell Division / drug effects
  • Cyclin B / antagonists & inhibitors
  • Cyclin-Dependent Kinases / antagonists & inhibitors*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • K562 Cells
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology*
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Cyclin B
  • Enzyme Inhibitors
  • Pyrazoles
  • Pyrimidines
  • pyrazolo(3,4-d)pyrimidine
  • CDC2 Protein Kinase
  • Cyclin-Dependent Kinases