Our laboratory is 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 both 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).
Herůdková, J.; Paruch, K.; Khirsariya, P.; Souček, K.; Krkoška, M.; Vondálová Blanářová, O.; Sova, P.; Kozubík, A.; Hyršlová Vaculová,A. Chk1 inhibitor SCH900776 effectively potentiates the cytotoxic effects of platinum-based chemotherapeutic drugs in human colon cancer cells. Neoplasia 2017, 19, 830.
Paculová, H.; Kramara, J.; Šimečková, Š.; Souček, K.; Hylse, O.; Paruch, K.; Svoboda, M.; Mistrik, M.; Kohoutek, J. BRCA1 or CDK12 loss sensitizes cells to CHK1 inhibitors. Tumor Biology 2017, accepted.
Samadder, P.; Suchánková, T.; Hylse, O.; Khirsariya, P.; Nikulenkov, F.; Drápela, S.; Straková, N.; Vaňhara, P.; Vašíčková, K.; Kolářová, H.; Binó, L.; Bittová, M.; Ovesná, P.; Kollár, P.; Fedr, R.; Ešner, M.; Jaroš, J.; Hampl, A.; Krejčí, L.; Paruch, K.; Souček, K. Synthesis and profiling of a novel potent selective inhibitor of CHK1 kinase possessing unusual N-trifluoromethylpyrazole pharmacophore resistant to metabolic N-dealkylation. Mol. Cancer Ther. 2017, 16, 1831.
Hylse, O.; Maier, L.; Kučera, R.; Perečko, T.; Svobodová, A.; Kubala, L.; Paruch, K.; Švenda, J. A concise synthesis of forskolin. Angew. Chem. Int. Ed. 2017, 41, 12586.
Maier, L.; Khirsariya, P.; Hylse, O.; Adla, S. K.; Černová, L.; Poljak, M.; Krajčovičová, S.; Weis, E.; Drápela, S.; Souček, K.; Paruch, K. Diastereoselective Flexible Synthesis of Carbocyclic C-nucleosides. J. Org. Chem. 2017, 82, 3382.
Nekardová, M.; Vymětalová, L.; Khirsariya, P.; Kováčová, S.; Hylsová, M.; Jorda, R.; Kryštof, V.; Fanfrlík, J.; Hobza, P.; Paruch, K. Structural basis of the interaction of cyclin-dependent kinase 2 with roscovitine and its analogues having bioisosteric central heterocycles. ChemPhysChem 2017, 18, 785.
Chalupa, D.; Vojáčková, P.; Partl, J.; Pavlovič, D.; Nečas, M.; Švenda, J. Enantioselective synthesis of cephalimysins B and C. Org. Lett. 2017, 19, 750.
Hylsová, M.; Carbain, B.; Fanfrlík, J.; Musilová, L.; Haldar, S.; Köprülüoğlu, C.; Ajani, H.; Brahmkshatriya, P. S.; Jorda, R.; Kryštof, V.; Hobza, P.; Echalier, A.; Paruch, K.; Lepšík, M. Explicit Treatment of Active-site Waters Enhances Quantum Mechanical/Implicit Solvent Scoring: Inhibition of CDK2 by New Pyrazolo[1,5-a]Pyrimidines. Eur. J. Med. Chem. 2017, 126, 1118.
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