Synthesis and properties of some novel anti-calmodulin drugs.

Abstract

The preparation and properties of some novel inhibitors of calmodulin function are described. The compounds are cationic derivatives of phenyl-substituted thiazoles which inhibit the calmodulin stimulation of cyclic-AMP phosphodiesterase and are active against animal tumor cells in culture. These derivatives form the basis for the preparation of new, more potent inhibitors of calmodulin function which could take advantage of the reported elevated levels of calcium-bound calmodulin in tumor cells and show preferential anti-tumor activity.

• Authors: T T Sakai, N R Krishna
• Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 7 Issue 8 Pg. 1559-65 (Aug 1999) ISSN: 0968-0896 [Print] England
• PMID: 10482448 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Antineoplastic Agents
• Calmodulin
• Thiazoles
• 3',5'-Cyclic-AMP Phosphodiesterases

Topics

• 3',5'-Cyclic-AMP Phosphodiesterases (antagonists & inhibitors)
• Animals
• Antineoplastic Agents (chemical synthesis, metabolism, pharmacology)
• Calmodulin (antagonists & inhibitors, metabolism)
• Leukemia L1210 (pathology)
• Mice
• Protein Binding
• Thiazoles (chemical synthesis, metabolism, pharmacology)
• Tumor Cells, Cultured