The research in our laboratory focuses on development of synthetic methods and strategies for preparation of structurally non-trivial small molecules for applications in biomedical research. Specifically, our project includes:
Infrastructure for modern organic synthesis:
VOJÁČKOVÁ, P.; MICHALSKA, L.; NEČAS, M.; SHCHERBAKOV, D.; BOTTGER, E. C.; ŠPONER, J.; ŠPONER, J.; ŠVENDA, J. A Stereocontrolled Synthesis of (−)-Bactobolin A. J. Am. Chem. Soc. 2020, 142, 7306.
BOUDNÝ, M.; ZEMANOVÁ, J.; KHIRSARIYA, P.; BORSKÝ, M.; VERNER, J.; ČERNÁ, J.; OLTOVÁ, A.; ŠEDA, V.; MRÁZ, M.; JAROŠ, J.; Kašparková, M.; Jašková, Z.; Spunarová, M.; Brychtová, Y.; Souček, K.; Drápela, S.; Mayer, J.; Paruch, K.; Trbušek, M. Novel Chk1 inhibitor MU380 exhibits significant single-agent activity in TP53-mutated chronic lymphocytic leukemia cells. Haematologica 2019, 104, 2443.
NĚMEC, V.; HYLSOVÁ, M.; MAIER, L.; FLEGEL, J.; SIEVERS, S.; ZIEGLER, S.; SCHRÖDER, M. BERGER, B.-T.; CHAIKUAD, A.; VALČIKOVÁ, B.; ULDRIJAN, S.; DRÁPELA, S.; SOUČEK, K.; WALDMANN, H.; KNAPP, S.; PARUCH, K. Furo[3,2-b]pyridine: A novel privileged scaffold for highly selective kinase inhibitors and effective modulators of the Hedgehog pathway. Angew. Chem. Int. Ed. 2019, 58, 1062.
HAVEL, Š.; KHIRSARIYA, P.; AKAVARAM, N.; PARUCH, K.; CARBAIN, B. Preparation of 3,4-substituted-5-aminopyrazoles and 4-substituted-2-aminothiazoles. J. Org. Chem. 2018, 83, 15380.
VOJÁČKOVÁ, P.; ChALUPA, D.; PRIEBOJ, J.; NEČAS, M.; ŠVENDA, J. Enantioselective Conjugate Additions of 2-Alkoxycarbonyl-3(2H)-furanones. Org. Lett. 2018, 20, 7085.
Substituted furo [3,2-b]pyridines - new compounds with targeted biological activity which effectively inhibit the activity of PIM kinases. PIM kinases are proteins whose overproduction is characteristic for prostate cancer cells, and some forms of leukemia and lymphomas. Compounds can be used for prostate cancer treatment. The compounds are covered by Czech patentCZ 305472.