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STUDIES ON THE SYNTHESIS AND BIOLOGICAL ACTIVITY OF COLCHICINE ANALOGUES

Dominik S. Koszelewski ,  Ryszard Ostaszewski 

Polish Academy of Sciences, Institute of Physical Chemistry, Kasprzaka 44/52, Warszawa 01-224, Poland

Abstract

Colchicine (1) is an alkaloid isolated from the dried corns and seeds of Colchicum autumnale. It is important to note that colchicine binds to tubulin founded in leucocytes and inhibits the migration of the white blood cells into the inflamed area, causing reduction in pain and inflammation. In the course of our studies a new colchicine analogues, compounds 2 were synthesized. These compounds bears a structural resemblance to colchicine 2 and are potential inhibitors of tubulin polymerization.

bez__tytu__u_1.gif

General method for the synthesis of compounds 2 will be presented together with biological activity profiles of its selected derivatives.

Acknowledgements

This work was supported by Polish State Committee for Scientific Research, project PBZ-MIN-007/P04/2003.

 

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Submitted: 2006-01-31 16:16
Revised:   2009-06-07 00:44