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Items: 37

1.

CDK12 controls G1/S progression by regulating RNAPII processivity at core DNA replication genes.

Chirackal Manavalan AP, Pilarova K, Kluge M, Bartholomeeusen K, Rajecky M, Oppelt J, Khirsariya P, Paruch K, Krejci L, Friedel CC, Blazek D.

EMBO Rep. 2019 Sep;20(9):e47592. doi: 10.15252/embr.201847592. Epub 2019 Jul 25.

2.

Synthesis and in Vitro Antimicrobial Activity Screening of New 3-Acetyl-2,5-disubstituted-1,3,4-oxadiazoline Derivatives.

Popiołek Ł, Biernasiuk A, Paruch K, Malm A, Wujec M.

Chem Biodivers. 2019 Jun;16(6):e1900082. doi: 10.1002/cbdv.201900082. Epub 2019 May 3.

PMID:
31050208
3.

Novel CHK1 inhibitor MU380 exhibits significant single-agent activity in TP53-mutated chronic lymphocytic leukemia cells.

Boudny M, Zemanova J, Khirsariya P, Borsky M, Verner J, Cerna J, Oltova A, Seda V, Mraz M, Jaros J, Jaskova Z, Spunarova M, Brychtova Y, Soucek K, Drapela S, Kasparkova M, Mayer J, Paruch K, Trbusek M.

Haematologica. 2019 Apr 11. pii: haematol.2018.203430. doi: 10.3324/haematol.2018.203430. [Epub ahead of print]

4.

EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology.

Brennecke P, Rasina D, Aubi O, Herzog K, Landskron J, Cautain B, Vicente F, Quintana J, Mestres J, Stechmann B, Ellinger B, Brea J, Kolanowski JL, Pilarski R, Orzaez M, Pineda-Lucena A, Laraia L, Nami F, Zielenkiewicz P, Paruch K, Hansen E, von Kries JP, Neuenschwander M, Specker E, Bartunek P, Simova S, Leśnikowski Z, Krauss S, Lehtiö L, Bilitewski U, Brönstrup M, Taskén K, Jirgensons A, Lickert H, Clausen MH, Andersen JH, Vicent MJ, Genilloud O, Martinez A, Nazaré M, Fecke W, Gribbon P.

SLAS Discov. 2019 Mar;24(3):398-413. doi: 10.1177/2472555218816276. Epub 2019 Jan 7.

PMID:
30616481
5.

Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway.

Němec V, Hylsová M, Maier L, Flegel J, Sievers S, Ziegler S, Schröder M, Berger BT, Chaikuad A, Valčíková B, Uldrijan S, Drápela S, Souček K, Waldmann H, Knapp S, Paruch K.

Angew Chem Int Ed Engl. 2019 Jan 21;58(4):1062-1066. doi: 10.1002/anie.201810312. Epub 2018 Dec 20.

PMID:
30569600
6.

Preparation of 3,4-Substituted-5-Aminopyrazoles and 4-Substituted-2-Aminothiazoles.

Havel S, Khirsariya P, Akavaram N, Paruch K, Carbain B.

J Org Chem. 2018 Dec 21;83(24):15380-15405. doi: 10.1021/acs.joc.8b02655. Epub 2018 Dec 6.

PMID:
30458618
7.

Flow Cytometric Analysis of Nucleoside Transporters Activity in Chemoresistant Prostate Cancer Model.

Drápela S, Fedr R, Khirsariya P, Paruch K, Svoboda M, Souček K.

Klin Onkol. Spring 2018;31(Supplementum1):140-144.

PMID:
29808688
8.

Synthesis and in vitro antimicrobial activity screening of new pipemidic acid derivatives.

Popiołek Ł, Biernasiuk A, Paruch K, Malm A, Wujec M.

Arch Pharm Res. 2018 Jun;41(6):633-645. doi: 10.1007/s12272-018-1025-3. Epub 2018 Apr 4.

9.

Impact of the access tunnel engineering on catalysis is strictly ligand-specific.

Kaushik S, Marques SM, Khirsariya P, Paruch K, Libichova L, Brezovsky J, Prokop Z, Chaloupkova R, Damborsky J.

FEBS J. 2018 Apr;285(8):1456-1476. doi: 10.1111/febs.14418. Epub 2018 Mar 25.

10.

BRCA1 or CDK12 loss sensitizes cells to CHK1 inhibitors.

Paculová H, Kramara J, Šimečková Š, Fedr R, Souček K, Hylse O, Paruch K, Svoboda M, Mistrík M, Kohoutek J.

Tumour Biol. 2017 Oct;39(10):1010428317727479. doi: 10.1177/1010428317727479.

PMID:
29025359
11.

Chk1 Inhibitor SCH900776 Effectively Potentiates the Cytotoxic Effects of Platinum-Based Chemotherapeutic Drugs in Human Colon Cancer Cells.

Herůdková J, Paruch K, Khirsariya P, Souček K, Krkoška M, Vondálová Blanářová O, Sova P, Kozubík A, Hyršlová Vaculová A.

Neoplasia. 2017 Oct;19(10):830-841. doi: 10.1016/j.neo.2017.08.002. Epub 2017 Sep 6.

12.

A Concise Synthesis of Forskolin.

Hylse O, Maier L, Kučera R, Perečko T, Svobodová A, Kubala L, Paruch K, Švenda J.

Angew Chem Int Ed Engl. 2017 Oct 2;56(41):12586-12589. doi: 10.1002/anie.201706809. Epub 2017 Sep 5.

PMID:
28782270
13.

Synthesis and Profiling of a Novel Potent Selective Inhibitor of CHK1 Kinase Possessing Unusual N-trifluoromethylpyrazole Pharmacophore Resistant to Metabolic N-dealkylation.

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.

Mol Cancer Ther. 2017 Sep;16(9):1831-1842. doi: 10.1158/1535-7163.MCT-17-0018. Epub 2017 Jun 15.

14.

Diastereoselective Flexible Synthesis of Carbocyclic C-Nucleosides.

Maier L, Khirsariya P, Hylse O, Adla SK, Černová L, Poljak M, Krajčovičová S, Weis E, Drápela S, Souček K, Paruch K.

J Org Chem. 2017 Apr 7;82(7):3382-3402. doi: 10.1021/acs.joc.6b02594. Epub 2017 Mar 20.

PMID:
28267331
15.

Structural Basis of the Interaction of Cyclin-Dependent Kinase 2 with Roscovitine and Its Analogues Having Bioisosteric Central Heterocycles.

Nekardová M, Vymětalová L, Khirsariya P, Kováčová S, Hylsová M, Jorda R, Kryštof V, Fanfrlík J, Hobza P, Paruch K.

Chemphyschem. 2017 Apr 5;18(7):785-795. doi: 10.1002/cphc.201601319. Epub 2017 Feb 15.

PMID:
28128514
16.

Explicit treatment of active-site waters enhances quantum mechanical/implicit solvent scoring: Inhibition of CDK2 by new pyrazolo[1,5-a]pyrimidines.

Hylsová M, Carbain B, Fanfrlík J, Musilová L, Haldar S, Köprülüoğlu C, Ajani H, Brahmkshatriya PS, Jorda R, Kryštof V, Hobza P, Echalier A, Paruch K, Lepšík M.

Eur J Med Chem. 2017 Jan 27;126:1118-1128. doi: 10.1016/j.ejmech.2016.12.023. Epub 2016 Dec 11.

PMID:
28039837
17.

Chk1 inhibition significantly potentiates activity of nucleoside analogs in TP53-mutated B-lymphoid cells.

Zemanova J, Hylse O, Collakova J, Vesely P, Oltova A, Borsky M, Zaprazna K, Kasparkova M, Janovska P, Verner J, Kohoutek J, Dzimkova M, Bryja V, Jaskova Z, Brychtova Y, Paruch K, Trbusek M.

Oncotarget. 2016 Sep 20;7(38):62091-62106. doi: 10.18632/oncotarget.11388.

18.

Site-specific analysis of protein hydration based on unnatural amino acid fluorescence.

Amaro M, Brezovský J, Kováčová S, Sýkora J, Bednář D, Němec V, Lišková V, Kurumbang NP, Beerens K, Chaloupková R, Paruch K, Hof M, Damborský J.

J Am Chem Soc. 2015 Apr 22;137(15):4988-92. doi: 10.1021/jacs.5b01681. Epub 2015 Apr 9.

PMID:
25815779
19.

Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.

Dwyer MP, Keertikar K, Paruch K, Alvarez C, Labroli M, Poker C, Fischmann TO, Mayer-Ezell R, Bond R, Wang Y, Azevedo R, Guzi TJ.

Bioorg Med Chem Lett. 2013 Nov 15;23(22):6178-82. doi: 10.1016/j.bmcl.2013.08.110. Epub 2013 Sep 7.

PMID:
24091081
20.

Are time-dependent fluorescence shifts at the tunnel mouth of haloalkane dehalogenase enzymes dependent on the choice of the chromophore?

Amaro M, Brezovský J, Kováčová S, Maier L, Chaloupková R, Sýkora J, Paruch K, Damborský J, Hof M.

J Phys Chem B. 2013 Jul 3;117(26):7898-906. doi: 10.1021/jp403708c. Epub 2013 Jun 20.

PMID:
23781851
21.

Quantum mechanical scoring: structural and energetic insights into cyclin-dependent kinase 2 inhibition by pyrazolo[1,5-a]pyrimidines.

Brahmkshatriya PS, Dobeš P, Fanfrlik J, Rezáç J, Paruch K, Bronowska A, Lepšík M, Hobza P.

Curr Comput Aided Drug Des. 2013 Mar;9(1):118-29.

PMID:
23157414
22.

Cyclin-dependent kinase inhibitors inspired by roscovitine: purine bioisosteres.

Jorda R, Paruch K, Krystof V.

Curr Pharm Des. 2012;18(20):2974-80. Review.

PMID:
22571665
23.

Targeting the replication checkpoint using SCH 900776, a potent and functionally selective CHK1 inhibitor identified via high content screening.

Guzi TJ, Paruch K, Dwyer MP, 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.

Mol Cancer Ther. 2011 Apr;10(4):591-602. doi: 10.1158/1535-7163.MCT-10-0928. Epub 2011 Feb 14.

24.

Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 1.

Dwyer MP, Paruch K, Labroli M, Alvarez C, Keertikar KM, Poker C, Rossman R, Fischmann TO, Duca JS, Madison V, Parry D, Davis N, Seghezzi W, Wiswell D, Guzi TJ.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):467-70. doi: 10.1016/j.bmcl.2010.10.113. Epub 2010 Oct 27.

PMID:
21094608
25.

Discovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: a template-based approach--part 2.

Labroli M, Paruch K, Dwyer MP, Alvarez C, Keertikar K, Poker C, Rossman R, Duca JS, Fischmann TO, Madison V, Parry D, Davis N, Seghezzi W, Wiswell D, Guzi TJ.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):471-4. doi: 10.1016/j.bmcl.2010.10.114. Epub 2010 Oct 28.

PMID:
21094607
26.

Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.

Paruch K, Dwyer MP, Alvarez C, Brown C, Chan TY, Doll RJ, Keertikar K, Knutson C, McKittrick B, Rivera J, Rossman R, Tucker G, Fischmann T, Hruza A, Madison V, Nomeir AA, Wang Y, Kirschmeier P, Lees E, Parry D, Sgambellone N, Seghezzi W, Schultz L, Shanahan F, Wiswell D, Xu X, Zhou Q, James RA, Paradkar VM, Park H, Rokosz LR, Stauffer TM, Guzi TJ.

ACS Med Chem Lett. 2010 May 17;1(5):204-8. doi: 10.1021/ml100051d. eCollection 2010 Aug 12.

27.

Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor.

Parry D, Guzi T, Shanahan F, Davis N, Prabhavalkar D, Wiswell D, Seghezzi W, Paruch K, Dwyer MP, Doll R, Nomeir A, Windsor W, Fischmann T, Wang Y, Oft M, Chen T, Kirschmeier P, Lees EM.

Mol Cancer Ther. 2010 Aug;9(8):2344-53. doi: 10.1158/1535-7163.MCT-10-0324. Epub 2010 Jul 27.

28.

Structure-guided discovery of cyclin-dependent kinase inhibitors.

Fischmann TO, Hruza A, Duca JS, Ramanathan L, Mayhood T, Windsor WT, Le HV, Guzi TJ, Dwyer MP, Paruch K, Doll RJ, Lees E, Parry D, Seghezzi W, Madison V.

Biopolymers. 2008 May;89(5):372-9.

PMID:
17937404
29.

Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.

Paruch K, Dwyer MP, Alvarez C, Brown C, Chan TY, Doll RJ, Keertikar K, Knutson C, McKittrick B, Rivera J, Rossman R, Tucker G, Fischmann TO, Hruza A, Madison V, Nomeir AA, Wang Y, Lees E, Parry D, Sgambellone N, Seghezzi W, Schultz L, Shanahan F, Wiswell D, Xu X, Zhou Q, James RA, Paradkar VM, Park H, Rokosz LR, Stauffer TM, Guzi TJ.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6220-3. Epub 2007 Sep 8.

PMID:
17904841
30.

Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors.

Dwyer MP, Paruch K, Alvarez C, Doll RJ, Keertikar K, Duca J, Fischmann TO, Hruza A, Madison V, Lees E, Parry D, Seghezzi W, Sgambellone N, Shanahan F, Wiswell D, Guzi TJ.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6216-9. Epub 2007 Sep 8.

PMID:
17904366
31.

Inhibitors of the NTPase/helicases of hepatitis C and related Flaviviridae viruses.

Bretner M, Najda A, Podwińska R, Baier A, Paruch K, Lipniacki A, Piasek A, Borowski P, Kulikowski T.

Acta Pol Pharm. 2004 Dec;61 Suppl:26-8.

32.

Functionalizations of [6]- and [7]helicenes at their most sterically hindered positions.

Paruch K, Vyklický L, Wang DZ, Katz TJ, Incarvito C, Zakharov L, Rheingold AL.

J Org Chem. 2003 Oct 31;68(22):8539-44.

PMID:
14575483
33.

[Evaluation of surgical treatment results of coarctation of the aorta in neonates and young infants].

Paruch K, Weryński P, Szydłowski L, Rudziński A, Malec E.

Przegl Lek. 2002;59(9):744-6. Polish.

PMID:
12632901
34.

First friedel-crafts diacylation of a phenanthrene as the basis for an efficient synthesis of nonracemic

Paruch K, Katz TJ, Incarvito C, Lam KC, Rhatigan B, Rheingold AL.

J Org Chem. 2000 Nov 3;65(22):7602-8.

PMID:
11076621
35.

Why (1S)-Camphanates Are Excellent Resolving Agents for Helicen-1-ols and Why They Can Be Used to Analyze Absolute Configurations.

Thongpanchang T, Paruch K, Katz TJ, Rheingold AL, Lam KC, Liable-Sands L.

J Org Chem. 2000 Mar 24;65(6):1850-1856.

PMID:
10814159
37.

[Diagnostic problems in atresia and hypoplasia of the aortic arch with systemic right ventricle].

Olczykowska-Siara E, Paruch K, Szydłowski L.

Pediatr Pol. 1983 Jun;58(6):537-42. Polish. No abstract available.

PMID:
6646912

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