2017

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.

2016

Zemanová, J.; Hylse, O.; Collaková, J.; Veselý, P.; Oltová, A.; Borský, M.; Zápražná, K.; Kašpárková, M.; Janovská, P.; Verner, J.; Kohoutek, J.; Dzimková, M.; Bryja, V.; Jaskova, Z.; Brychtová, Y.; Paruch, K.; Trbušek, M. Chk1 inhibition significantly potentiates activity of nucleoside analogs in TP53-mutated B-lymphoid cells. Oncotarget 2016, 7, 6209.

Hill, N.; Paruch, K.; Švenda, J. Late-stage annulative convergency in natural product synthesis. Tetrahedron 2016, 72, 3345.

2015

Damborsky, J.; Nikulenkov, F.; Sisáková, A.; Havel, Š.; Krejčí, L.; Carbain, B.; Brezovsky, J.; Daniel, L.; Paruch, K. Pyrazolotriazines as Inhibitors of Nucleases PCT Int. Appl. (2015), WO 2015/192817 A1.

Paruch, K.; Petrůjová, M.; Němec, V. Furopyridines as inhibitors of protein kinases PCT Int. Appl. (2015), WO 2015165428 A1. 

Paruch, K.; Petrůjová, M. Substituted Furo[3,2-b]pyridines Intended for Use as Medicaments (2015). Patent No. CZ 305472

Kučera, R.; Hylse, O.; Babiak, M.; Švenda, J. Facile rearrangements of a vinylogous alpha-hydroxy-beta-dicarbonyl substrate involving an apparent oxirane C-C bond scission. Tetrahedron Lett. 2015, 56, 6171.

Kováčová, S.; Adla, S. K.; Maier, L.; Babiak, M.; Mizushina, Y.; Paruch, K. Synthesis of carbocyclic analogs of dehydroaltenusin: Identification of a stable inhibitor of calf DNA polymerase alpha. Tetrahedron 2015, 71, 7575.

Amaro, M.; Brezovský, J.; Kováčová, S.; Sýkora, J.; Bednář, D.; Němec, V.; Lišková, V.; Kurumbang, N.; Beerens, K.; Chaloupková, R.; Paruch, K.; Hof, M.; Damborský, J. Site-specific Analysis of Protein Hydration Based on Unnatural Amino Acid Fluorescence. J. Am. Chem. Soc. 2015, 137, 4988.

2014

Maier, L.; Hylse, O.; Nečas, M.; Trbušek, M.; Ytre-Arne, M.; Dalhus, B.; Bjorås, M.; Paruch, K.New Carbocyclic Nucleosides: Synthesis of Carbocyclic Pseudoisocytidine and its Analogs. Tetrahedron Lett. 2014, 55, 3713.

2013

Amaro, M.; Brezovsky, J.; Kovacova, S.; Maier, L.; Chaloupkova, R.; Sykora, J.; Paruch, K.; Damborsky, J.; Hof, M. Are Time-Dependent Fluorescence Shifts at the Tunnel Mouth of Haloalkane Dehalogenase Enzymes Dependent on the Choice of the Chromophore? J. Phys. Chem. B 2013, 117, 7898.

Brahmkshatriya, P. S.; Dobes, P.; Fanfrlik, J.; Rezac, J.; Paruch, K.; Bronowska, A.; Lepsik, M.; Hobza, P. Quantum Mechanical Scoring: Structural and Energetic Insights into Cyclin-Dependent Kinase 2 Inhibition by Pyrazolo[1,5-a]pyrimidinesCurr. Comput. Aided Drug Des. 2013, 9, 118-129.

2012

Jorda, R.; Paruch, K.; Krystof, V. Cyclin-dependent Kinase Inhibitors Inspired by Roscovitine: Purine Bioisosteres. Curr. Pharm. Design 2012, 18, 2974.

 

Previous publications

Švenda, J.; Sheremet, M.; Kremer, L.; Maier, L.; Bauer, J. O.; Strohmann, C.; Ziegler, S.; Kumar, K.; Waldmann, H. Biology-Oriented Synthesis of a Withanolide-Inspired Compound Collection Reveals Novel Modulators of Hedgehog Signalling. Angew. Chem. Int. Ed. Engl. 2015 DOI: 10.1002/ange.201500112.

Labroli, M.; Dwyer, M. P.; Shen, R.; Popovici-Muller, J.; Pu, Q.; Richard, J.; Rosner, K.; Paruch, K.; Guzi, T. J. Syntheses of 5´-amino-2´,5´-dideoxy-2´,2´-difluorocytidine Derivatives as Novel Anticancer Nucleoside Analogs. Tetrahedron Lett. 2014, 55, 598.

Dwyer, M. P.; Keertikar, K.; Paruch, K.; Alvarez, C.; Labroli, M.; Poker, C.; Fischmann, T. O.; Mayer-Ezell, R.; Bond, R.; Wang, Y.; Azevedo, R.; Guzi, T. J. Discovery of Pyrazolo[1,5- a]pyrimidine-based Pim Inhibitors: A Template-Based Approach.Bioorg. Med. Chem. Lett. 2013, 23, 6178.

Smaltz, D.; Švenda, J., Myers, A. G. Diastereoselective Additions of Allylmetal Reagents to Free and Protected syn-a,b-Dihydroxyketones Enable Efficient Synthetic Routes to Methyl Trioxacarcinoside A. Org. Lett. 2012, 14, 1812.

Švenda, J.; Hill, N. D.; Myers, A. G. A Multiply Convergent Platform for the Synthesis of Trioxacarcins. Proc. Natl. Acad. Sci. U.S.A. 2011, 108, 6709.

Guzi, T.; Paruch, K.; Dwyer, M.; Labroli, M.; Shanahan, F.; Davis, N.; Taricani, L.; Wiswell, D.; Seghezzi, W.; Penaflor, E.; Bhagwat, B.; Wang, W.; Gu, D.;  Hsieh, Y.; Lee, S.; Liu, M.; Parry, D. Targeting the Replication Checkpoint Using SCH 900776, a Potent and Functionally Selective CHK1 Inhibitor Identified Via High Content Screening. Mol. Cancer Ther. 2011, 10, 591.

Labroli, M.; Paruch, K..; Dwyer, M. P.; Alvarez, C.; Keertikar, K. M;. Poker, C.; Rossman, R.; Fischmann, T. O.; Duca, J. S.; Madison, V.; Parry, D.; Davis, N.; Seghezzi, W.; Wiswell, D.; Guzi, T. J. Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 2. Bioorg. Med. Chem. Lett. 2011, 21, 471.

Dwyer, M. P.; Paruch, K.; Labroli, M.; Alvarez, C.; Keertikar, K. M;. Poker, C.; Rossman, R.; Fischmann, T. O.; Duca, J. S.; Madison, V.; Parry, D.; Davis, N.; Seghezzi, W.; Wiswell, D.; Guzi, T. J. Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 1. Bioorg. Med. Chem. Lett. 2011, 21, 467.

Parry, D.; Guzi, T. J.; Shanahan, F.; Davis, N.; Prabhavalkar, D.; Wiswell, D; Seghezzi, W.; Paruch, K.; Dwyer, M. P.; Doll, R. J.; Nomeir, A. A.; Windsor, W.; Fischmann, T.; Wang, Y.; Oft, M.; Chen, T.; Kirschmeier, P.; Lees, E. M. Dinaciclib (SCH 727965), a Novel and Potent Cyclin-Dependent Kinase Inhibitor. Mol. Cancer Ther. 2010, 9, 2344.

Paruch, K.; Dwyer, M. P.; Alvarez, C.; Brown, C.; Chan T.-Y.; Doll, R. J.; Keertikar K.; Knutson, C.; McKittrick, B.; Rivera, J.; Rossman, R.; Tucker, G.; Fishmann, T.; Hruza, A.; Madison, V.; Nomeir, A. A.; Wang, Y.; Kirschmeier, P.; Lees, E.; Parry, D.; Sgambellone, N.; Seghezzi, W.; Schultz, L.; Shanahan, F.; Wiswell, D.; Xu, X.; Zhou, Q.; James, R. A.; Paradkar, V. M.; Park, H.; Rokosz, L. R.; Stauffer, T. M.; Guzi, T. J.  Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.  ACS Med. Chem. Lett. 2010, 1, 204.

Švenda, J.; Myers, A. G. Anti-Selective Epoxidation of Methyl a-Methylene-b-tert-Butyldimethylsilyloxycarboxylate Esters. Evidence for Stereospecific Oxygen Atom Transfer in a Nucleophilic Epoxidation Process. Org. Lett. 2009, 11, 2437. 

Fischmann, T. O.; Hruza, A.; Duca, J. S.; Ramanathan, L.; Mayhood, T.; Windsor, W. T.; Le, H. V.; Guzi, T. J.; Dwyer, M. P.; Paruch, K.; Doll, R. J.; Lees, E.; Parry, D.; Seghezzi, W.; Madison, V.  Structure-Guided Discovery of Cyclin-Dependent Kinase Inhibitors.  Biopolymers 2008, 89, 372.

Dwyer, M. P.; Paruch, K.; Alvarez, C.; Doll, R. J.; Keertikar, K.; Duca, J.; Fischmann, T.; Hruza, A.; Madison, V.; Lees, E.; Parry, D.; Sgambellone, N.; Seghezzi, W.; Shanahan, F.; Wiswell, D.; Guzi, T. J.  Versatile Templates for the Development of Novel Kinase Inhibitors: Discovery of Novel CDK  Inhibitors.  Bioorg. Med. Chem. Lett. 2007, 17, 6216.

Paruch, K.; Dwyer, M. P.; Alvarez, C.; Brown, C.; Chan, T.-Y.; Doll, R. J.; Keertikar, K.; Knutson, C.; McKittrick, B.; Rivera, J.; Rossman, R.; Tucker, G.; Fischmann, T.; Hruza, A.; Madison, V.; Nomeir, A. A.; Wang, Y.; Lees, E.; Parry, D.; Sgambellone, N.; Seghezzi, W.; Schultz, L.; Shanahan, F.; Wiswell, D.; Xu, X.; Zhou, Q.; James, R. A.; Paradkar, V. M.; Park, H.; Rokosz, L. R.; Stauffer, T. M.; Guzi, T. J.  Pyrazolo[1,5-a]pyrimidines as Orally Available Inhibitors of Cyclin-Dependent Kinase 2.  Bioorg. Med. Chem. Lett. 2007, 17, 6220.

Bower, J. F.; Chakthong, S.; Švenda, J.; Williams, A. J.; Lawrence, R. M.; Szeto, P.; Gallagher, T. Reactivity of Cyclic Sulfamidates Towards Sulfur-Stabilized Enolates. Stereocontrolled Synthesis of Functionalized Lactams. Org. Biomol. Chem. 2006, 4, 1868.

Bower, J. F.; Švenda, J.; Williams, A. J.; Charmant, J. P. H.; Lawrence, R. M.; Szeto, P.; Gallagher, T. Cyclic Sulfamidates as Vehicles for the Synthesis of Substituted Lactams. Org. Lett. 2004, 6, 4727.

Paruch, K.; Vyklicky, L.; Wang, Z.; Katz, T. J.; Incarvito, C.; Zakharov, L.; Rheingold, A. Functionalizations of [6]- and [7]-Helicenes at their Most Sterically Hindered Positions. J. Org. Chem. 2003, 68, 8539.

Paruch, K.; Vyklicky, L.; Katz, T. J. Helicenebisquinones: Synthesis of a [7]Helicenebisquinone.  Org. Syntheses 2003, 80, 233.

Paruch, K.; Vyklicky, L.; Katz, T. J. Preparation  of 9,10-Dimethoxyphenanthrene and 3,6-Diacetyl-9,10-dimethoxyphenanthrene.  Org. Syntheses 2003, 80, 227.

Paruch, K.; Vyklicky, L.; Katz, T. J.; Incarvito, C.; Rheingold, A. Expeditious Procedure To Synthesize Ethers and Esters of Tri- and Tetrahydroxy[6]helicenebisquinones from the Dye-Intermediates Disodium 4-Hydroxy- and 4,5-Dihydroxynaphthalene-2,7-disulfonates. J. Org. Chem. 2000, 65, 8774.

Paruch, K.; Katz, T. J.; Incarvito, C.; Lam, K.-C.; Rhatigan, B.; Rheingold, A. First Friedel-Crafts Diacylation of a Phenanthrene as the Basis for an Efficient Synthesis of Nonracemic [7]Helicenes. J. Org. Chem. 2000, 65, 7602.

Thongpanchang, T.; Paruch, K.; Katz, T. J.; Rheingold, A.; Lam, K.-C.; Liable-Sands, L. Why (1S)-Camphanates Are Excellent Resolving Agents for Helicen-1-ols and Why They can Be Used to Analyze Absolute Configurations.  J. Org. Chem. 2000, 65, 1805.

Dreher, S. D.; Paruch, K.; Katz, T. J. Acidified Alcohols as Agents to Introduce and Exchange Alkoxyls on the Periphery of Helicenes.  J. Org. Chem. 2000, 65, 806.