Laboratories of Organic Synthesis and Medicinal Chemistry

PIs: Mgr. Kamil Paruch, Ph.D. and Mgr. Jakub Švenda, Ph.D.
website: http://www.orgsyn.sci.muni.cz

 

Our laboratories are focused on the development of synthetic methods and strategies for the preparation of structurally non-trivial organic molecules for applications in biomedical research. We target man-made and naturally occurring bioactive molecules that feature underexplored pharmacophores and/or structural complexity challenging the current state-of-the-art in organic synthesis. Our target compounds are profiled in close collaboration with top-class Czech and international biologists. Research areas of interest include small-molecule modulation of selected human kinases, adenylyl cyclases, and nucleases.    

Students in our laboratory have an opportunity to explore challenging problems in experimental chemistry research and to gain a solid knowledge of modern organic synthesis. Regular interactions with biologists expose our students to the interdisciplinary nature of modern research in life sciences. 

Our lab is also part of the International Clinical Research Centre of St. Anne´s University Hospital in Brno and Mayo Clinic in Rochester (USA).

Research Topics

  • Highly selective inhibitors of kinases
  • Natural product synthesis
  • Development of tools for chemical biology

Selected Publications

A Platform for the Synthesis of Oxidation Products of Bilirubin. Mujawar, T.; Sevelda, P.; Madea, D.; Klán, P.; Švenda, J.* J. Am. Chem. Soc. 2024, 146, 1603–1611.

Discovery of potent and exquisitely selective inhibitors of kinase CK1 with tunable isoform selectivity. Němec, V.; Khirsariya, P.; Janovská, P.; Martín Moyano, P.; Maier, L.; Lesáková, P.; Kebková, P.; Gybel’, T.; Berger, B.-T.; Chaikuad, A.; Reinecke, M.; Küster, B.; Knapp, S.; Bryja, V.*; Paruch, K.* Angew. Chem. Int. Ed. 2023, e202217532.

Convergent Assembly of the Tricyclic Labdane Core Enables Synthesis of Diverse Forskolin-like Molecules. Szczepanik, P. M.; Mikhaylov, A. A.; Hylse, O.; Kučera, R.; Daďová, P.; Nečas, M.; Kubala, L.; Paruch, K.; Švenda, J.* Angew. Chem. Int. Ed. 2023, 62, e202213183.

Short synthesis of (+)-actinobolin: Simple entry to complex small-molecule inhibitors of protein synthesis. Tharra, P. R.; Mikhaylov, A.; Švejkar, J.; Gysin, M.; Hobbie, S. N.; Švenda, J.* Angew. Chem. Int. Ed. 2022, 61, e202116520.

CDK11 is a key regulator mediating pre-mRNA splicing by phosphorylation of SF3B1. Hluchý, M.; Gajdušková, P.; Ruiz de Los Mozos, I.; Rájecký, M.; Kluge, M.; Berger, B.-T.; Slabá, Z.; Potěšil, D.; Weis, E.; Ule, J.; Zdráhal, Z.; Knapp, S.; Paruch, K.; Friedel, C. C.; Blažek, D.* Nature 2022, 609, 829.

Synthesis and profiling of highly selective inhibitors of methyltransferase DOT1L based on carbocyclic C-nucleosides. Khirsariya, P.; Pospíšil, P.; Maier, L.; Boudný, M.; Babáš, M.; Kroutil, O.; Mráz, M.; Vácha, R.; Paruch, K.*​ J. Med. Chem. 2022, 65, 5701.

 

  

laboratory of organic photochemistry laboratory of organic synthesis laboratory of organic synthesis and medicinal chemistry supramolecular chemistry group

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