Apoptosis-inducing activity of synthetic intermediates of halichlorine.

Abstract

Synthetic intermediates of alkaloid halichlorine with the azaspiro core structure have been found to induce apoptosis of cultured human cells including an acute monocytic leukemia cell line (THP-1) at micromolar concentrations. The novel biological activity of the intermediates was suggested to depend on the skeletal structure and silyloxymethyl functionality on the five-membered ring.

• Authors: Midori Itoh, Jun Kuwahara, Kohji Itoh, Yu ichi Fukuda, Mikiko Kohya, Mitsuru Shindo, Kozo Shishido
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 12 Issue 16 Pg. 2069-72 (Aug 19 2002) ISSN: 0960-894X [Print] England
• PMID: 12127506 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Alkaloids
• Chromatin
• Spiro Compounds
• halichlorine
• CASP3 protein, human
• CASP7 protein, human
• Caspase 3
• Caspase 7
• Caspases

Topics

• Alkaloids (chemical synthesis, chemistry, pharmacology)
• Animals
• Apoptosis (drug effects)
• Caspase 3
• Caspase 7
• Caspases (metabolism)
• Chromatin (drug effects, metabolism)
• Dose-Response Relationship, Drug
• Enzyme Activation (drug effects)
• Humans
• Molecular Structure
• Spiro Compounds (chemical synthesis, chemistry, pharmacology)
• Time Factors
• Tumor Cells, Cultured