Inhibition of Src kinase activity by 7-[(2,4-dichloro-5-methoxyphenyl)amino]-2-heteroaryl-thieno[3,2-b]pyridine-6-carbonitriles

Bioorg Med Chem Lett. 2005 Nov 1;15(21):4681-4. doi: 10.1016/j.bmcl.2005.07.061.

Abstract

7-[(2,4-Dichloro-5-methoxyphenyl)amino]thieno[3,2-b]pyridine-6-carbonitriles with various heteroaryl groups at C-2 are inhibitors of Src kinase activity. Of these new analogs, compounds substituted at C-2 by a 3,5-furan or a 2,5-pyridine had the best activity in the Src enzyme and cell assays.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Cell Line
  • Cell Line, Tumor
  • Humans
  • Inhibitory Concentration 50
  • Kinetics
  • Mice
  • Mice, Nude
  • Neoplasms, Experimental / drug therapy
  • Nitriles / chemical synthesis*
  • Nitriles / pharmacology
  • Nitriles / therapeutic use
  • Pharmacokinetics
  • Protein Kinase Inhibitors / chemical synthesis*
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use
  • Structure-Activity Relationship
  • src-Family Kinases / antagonists & inhibitors*

Substances

  • Antineoplastic Agents
  • Nitriles
  • Protein Kinase Inhibitors
  • src-Family Kinases