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Chemoenzymatic approach to the synthesis of bioactive tripeptide mimetics for treatment of cancer
|Ryszard Ostaszewski , Szymon Kłossowski , Michał Mroczkiewicz|
Institute of Organic chemistry of the Polish Academy of Sciences (ICHOPAS), Kasprzaka 44/52, Warsaw 01-224, Poland
Biocatalysis is a methodology of growing importance among organic chemists aiming at the synthesis of bioactive compounds, resulting in the establishment of many successful synthetic protocols. Main reason for this is an enormous selectivity of biocatalysts.
Tripeptides and tripeptide mimetics are widely investigated due to their biological activity. Among them, an anti-inflammatory agent 1, an antibiotic 2, and human rhinovirus 3C protease inhibitors can be found.
Tripeptides with C-terminal aldehyde group are of special interest. Compound 3 (Mg- 132) is a potent and selective inhibitor of 20S proteasome, which is often used as a reference in biomedical studies.
The results of our studies on the successful combination of mutlicomponent reactions with enzymatic transformations to the synthesis of bioactive tripeptide mimetics, will be presented [2,3,4].
 K. Faber. Biotransformations in Organic Chemistry - A Textbook. Springer-Verlag, Berlin, 5th edition, 2004.
 Szymanski, W., Ostaszewski, R.; Tetrahedron, 17, 2667-2671, 2006.
 Mroczkiewicz M., Ostaszewski R., Tetrahedron, 65, 4025-4034, 2009.
 Mroczkiewicz M.,Winkler K.,Nowis D.,Placha G.,Golab G.,Ostaszewski R., J. Med. Chem., 53, 1509–1518, 2010.
Presentation: Oral at VII Multidyscyplinarna Konferencja Nauki o Leku, by Ryszard Ostaszewski
See On-line Journal of VII Multidyscyplinarna Konferencja Nauki o Leku
Submitted: 2010-03-12 11:33 Revised: 2010-04-01 09:59