Name:

 

Milan Pour

 

 

 

Affiliation:

 

Laboratory of Structure and Interactions of Biologically Active Molecules, Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic

 

 

 

E-mail:

 

pour@faf.cuni.cz

 

 

 

Web:

 

http://www.faf.cuni.cz/

 

 

 

Research:

 

synthesis of biologically active natural products and their analogues, structure-activity relationships

 

 

 

Short CV:

 

1984-1989 MSc. in Organic Chemistry, Faculty of Science, Charles University, Prague, Czech Republic
 
1991-1994 Ph.D. with L. N. Mander, Research School of Chemistry, Australian National University, Canberra, Australia
 
1994-1996 postdoc with E. Negishi, Department of Chemistry, Purdue University, West Lafayette, Indiana, USA
 
1996-1999 Assistant Professor, Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Králové, Czech Republic
 
since 1999 Associate Professor of Organic Chemistry, Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Králové, Czech Republic
 

 

 

 

Awards:

 

1989 Award for the Best Diploma Thesis of the Year from Charles University Chancellor
 
2001 Alfred Bader Prize for Organic Chemistry from the Czech Chemical Society
 

 

 

 

Publications:

 

Pour M., Negishi E. Efficient and Selective Synthesis of Nakienone A Involving a Novel Protocol for α-Alkenylation of Ketones via Palladium-Catalysed Alkenyl-Alkenyl Coupling. Tetrahedron Lett. 38: 525-528 (1997).
 
Pour M., Willis A. C., Furber M., Mander L. N. Synthesis of 3,12-dihydroxy-9,15-cyclogibberellins. Tetrahedron Lett. 54: 13833-13850 (1998).
 
Pour M., Špulák M., Balšánek V., Kuneš J., Buchta V., Waisser K. 3-Phenyl-5-methyl-2H,5H-furan-2-ones: Tuning Antifungal Activity by Varying Substituents on the Phenyl Ring. Bioorg. Med. Chem. Lett. 10: 1893-1895 (2000).
 
Pour M., Špulák M., Buchta V., Kubanová P., Vopršalová M., Wsól V., Fáková H., Koudelka P., Pourová H., Schiller R. 3-Phenyl-5-acyloxymethyl-2H,5H-furan-2-ones: Synthesis and Biological Activity of a Novel Group of Potential Antifungal Drugs. J. Med. Chem. 44: 2701-2706 (2001).
 
Pour M., Špulák M., Balšánek V., Kuneš J., Buchta V. Synthesis and Structure-Antifungal Activity Relationships of 3-Aryl-5-alkyl-2,5-dihydrofuran-2-ones and Their Carbanalogues. Further Refinement of Tentative Pharmacophore Group. Bioorg. Med. Chem. 11: 2843-2866 (2003).
 

 

 

 

Research interest:

 

Biologically active natural products have often served as useful prototypes of pharmaceutical agents. However, a number of prospective drugs from the family of natural products are organic compounds of high complexity, accessible exclusively by way of multistep total synthesis. Since all potential drugs must be made in a practical fashion, this is a serious limitation in the development of new drugs based on natural product leads. On the other hand, the action of a compound on a subcellular level does not necessarily require the presence of all structural features built in its molecule. In a number of cases, the desired biological effect is caused by the combination of several substructural elements, usually termed as pharmacophore, such as polar groups in certain spatial arrangement, capable of interaction with biomacromolecules in the target organism. Hence, the preparation of purposefully designed, easy-to-make synthetic analogues that simplify the structure of a biologically active natural product is a distinct possibility, especially when biological investigation is likely to be hampered by the necessity to supply the material by an elaborate synthesis.
A number of natural products from the family of butenolides (incrustoporine, CR 377, uncinine and many others) and pentenolides (eg. podolactones) display interesting biological effects, such as antifungal activity and cytotoxicity. Our projects are focused on (1) total syntheses of selected natural products of these two classes in an efficient and chemically interesting fashion, using modern synthetic methods employing transition metal catalysis, (2) design and synthesis of analogues of natural butenolides and pentenolides, (3) biological evaluation of the compounds and (4) using the results of biological studies as a feedback in the development of drugs based on unsaturated lactones as lead compounds.