P. Kovar

发表

Synthesis and in-vitro biological activity of macrocyclic urea Chk1 inhibitors.

Philip J. Merta, Gaoquan Li, Z. Tao, 2007, Bioorganic & medicinal chemistry letters.

Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors.

Chang Park, Saul H Rosenberg, Gaoquan Li, 2006, Bioorganic & medicinal chemistry letters.

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

L. Lam, C. Tse, Cheol‐Min Park, 2013, Nature Medicine.

Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors.

P. Kovar, Zehan Chen, Haiying Zhang, 2006, Bioorganic & medicinal chemistry letters.

Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.

Chang Park, John Xue, Saul H Rosenberg, 2007, Journal of medicinal chemistry.

Potent and orally bioavailable noncysteine-containing inhibitors of protein farnesyltransferase.

S. Ng, D. Augeri, P. Kovar, 1999, Bioorganic & medicinal chemistry letters.

Synthesis and biological evaluation of 4'-(6,7-disubstituted-2,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-biphenyl-4-ol as potent Chk1 inhibitors.

Saul H Rosenberg, Philip J. Merta, Gaoquan Li, 2007, Bioorganic & medicinal chemistry letters.

Cyanopyridyl containing 1,4-dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: improving oral biovailability.

Philip J. Merta, Gaoquan Li, Z. Tao, 2007, Bioorganic & medicinal chemistry letters.

Discovery of 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2'-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors.

Philip J. Merta, Gaoquan Li, Z. Tao, 2007, Bioorganic & medicinal chemistry letters.

1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyanopyrazin-2-yl)ureas [correction of cyanopyrazi] as potent and selective inhibitors of Chk1 kinase: synthesis, preliminary SAR, and biological activities.

Gaoquan Li, P. Kovar, Zehan Chen, 2005, Journal of medicinal chemistry.

Discovery of a well-absorbed, efficacious renin inhibitor, A-74273.

P. Kovar, H. Kleinert, J. Polakowski, 1992, Hypertension.

Cardiovascular Effects and Hemodynamic Mechanism of Action of the Novel, Nonpeptidic Renin Inhibitor A‐74273 in Dogs

P. Kovar, H. Kleinert, J. Wessale, 1993, Journal of cardiovascular pharmacology.

Effects of renin inhibitor A-72517 on hemodynamics and cardiac function in sodium-depleted dogs.

P. Kovar, S. Rosenberg, H. Kleinert, 1993, American journal of hypertension.

Souers AJ, Leverson JD, Boghaert ER et al.ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med 19:202-208

L. Lam, C. Tse, Cheol‐Min Park, 2013 .

Inhibition of farnesyltransferase with A-176120, a novel and potent farnesyl pyrophosphate analogue.

S. Ng, P. Kovar, S. Rosenberg, 2000, European journal of cancer.

Potent inhibitors of protein farnesyltransferase: heteroarenes as cysteine replacements.

S. Ng, P. Kovar, S. Rosenberg, 1999, Bioorganic & medicinal chemistry letters.

A-432411, a novel indolinone compound that disrupts spindle pole formation and inhibits human cancer cell growth

Philip J. Merta, P. Kovar, Zehan Chen, 2005, Molecular Cancer Therapeutics.

THE INFLUENCE OF WATER EXTRACTS OF SELECTED TURFGRASS SPECIES ON GERMINATION AND INITIAL GROWTH OF POA ANNUA L.

P. Kovar, Ľ. Vozár, J. Jančovič, 2013 .

Effect of Alginite in the Form of ALGEXr 6 Preparation on the Biomass Formation and Antioxidant Activity of Some Medicinal Plants

P. Kovar, J. Šimková, V. Sedláčková, 2021, Agrobiodiversity for Improving Nutrition, Health and Life Quality.

Investigating Correlation between Availability of Free Time Facilities for Pupils and Their Educational Achievements while Exploiting Linked Data and Volunteered Geographic Information

P. Kovar, 2015 .

Dynamics of the nitrogen content in aboveground phytomass on the turf after fertilization of different forms of fertilizers

P. Kovar, Ľ. Vozár, J. Jančovič, 2017 .

Discovery of N-ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET bromodomain inhibitor with selectivity for the second bromodomain.

K. Longenecker, P. Kovar, L. Hasvold, 2020, Journal of medicinal chemistry.

Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors.

Philip J. Merta, Magdalena Przytulinska, P. Kovar, 2008, Bioorganic & medicinal chemistry letters.

Rapid colchicine competition-binding scintillation proximity assay using biotin-labeled tubulin.

S. Ng, P. Kovar, S. Rosenberg, 2000, BioTechniques.

Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors

C. Tse, K. Longenecker, P. Richardson, 2017, Molecular Cancer Therapeutics.

SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT).

Ana L. Aguirre, Mikkel A. Algire, C. Tse, 2017, Bioorganic & medicinal chemistry letters.

Novel sulfonate derivatives: potent antimitotic agents.

S. Ng, P. Kovar, S. L. Gwaltney, 2001, Bioorganic & medicinal chemistry letters.

Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax)

C. Tse, D. Anderson, Daniel J. Anderson, 2015, Cell Death and Disease.

Correction to Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity.

Scott A. Erickson, C. Tse, A. Petros, 2015, Journal of medicinal chemistry.

Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.

S. Davidsen, Eric F. Johnson, J. Wilsbacher, 2010, Bioorganic & medicinal chemistry letters.

Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).

S. Davidsen, Eric F. Johnson, J. Wilsbacher, 2007, Bioorganic & medicinal chemistry letters.

Effect of different mowing intensities on phytomass production of permanent grassland in a warm and an arid region

P. Kovar, Ľ. Vozár, Peter Hric, 2022, Acta fytotechnica et zootechnica.

Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions.

Eric F. Johnson, I. Akritopoulou‐Zanze, P. Kovar, 2011, Bioorganic & medicinal chemistry letters.

Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.

S. Ng, P. Kovar, S. Rosenberg, 2002, Bioorganic & medicinal chemistry letters.

Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.

Z. Tao, P. Kovar, Zehan Chen, 2007, Bioorganic & medicinal chemistry letters.

Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors.

Chang Park, Philip J. Merta, Z. Tao, 2007, Journal of medicinal chemistry.

Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors.

Saul H. Rosenberg, Chang Park, P. Kovar, 2006, Bioorganic & medicinal chemistry letters.

Discovery of a peptide-based renin inhibitor with oral bioavailability and efficacy.

P. Kovar, S. Rosenberg, H. Kleinert, 1992, Science.

Unique Effects of Alginite as a Bituminous Rock on Soil, Water, Plants and Animal Organisms – Review

P. Kovar, O. Grygorieva, J. Brindza, 2021, Agrobiodiversity for Improving Nutrition, Health and Life Quality.

Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy

Dolores Diaz, Jun Chen, Deepak Sampath, 2015, Science Translational Medicine.

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.

A. Petros, Chaohong Sun, P. Kovar, 2017, Journal of medicinal chemistry.

Novel sulfonate analogues of combretastatin A-4: potent antimitotic agents.

S. Ng, P. Kovar, S. L. Gwaltney, 2001, Bioorganic & medicinal chemistry letters.

Studies directed toward the design of orally active renin inhibitors. 2. Development of the efficacious, bioavailable renin inhibitor (2S)-2-benzyl-3- [[(1-methylpiperazin-4-yl)sulfonyl]propionyl]-3-thiazol-4-yl-L-alanine amide of (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane (A-7251

P. Kovar, S. Rosenberg, J. Polakowski, 1993, Journal of medicinal chemistry.

Selective Chk1 inhibitors differentially sensitize p53‐deficient cancer cells to cancer therapeutics

Zhan Xiao, John Xue, Saul H Rosenberg, 2006, International journal of cancer.

Kinase Drug Discovery by Affinity Selection/Mass Spectrometry (ASMS): Application to DNA Damage Checkpoint Kinase Chk1

Hua Tang, Mark E Schurdak, Michael Coen, 2006, Journal of biomolecular screening.

Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.

Scott A. Erickson, C. Tse, A. Petros, 2015, Journal of medicinal chemistry.

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.

Brian J. Smith, C. Tse, A. Petros, 2014, ACS medicinal chemistry letters.

Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.

Scott A. Erickson, S. Davidsen, K. Swinger, 2010, Bioorganic & medicinal chemistry letters.

Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.

Chang Park, Saul H Rosenberg, Y. Tong, 2007, Bioorganic & medicinal chemistry.

The changes of the assimilation pigments content of turf Festuca spp. leaves after application of different nutrition forms

P. Kovar, Ľ. Vozár, Peter Hric, 2018 .

Controlling cellular distribution of drugs with permeability modifying moieties.

P. Richardson, A. Vasudevan, J. Wilsbacher, 2019, MedChemComm.

1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies.

Philip J. Merta, Z. Tao, Y. Tong, 2007, Bioorganic & medicinal chemistry letters.

The effect of Stockosorb® 500 Micro on the growth-production process of Festuca arundinacea Schreb.

P. Kovar, Ľ. Vozár, Peter Hric, 2018, Acta fytotechnica et zootechnica.

The turfs quality of selected Slovak varieties of the genus Festuca under the conditions without irrigation

P. Kovar, Ľ. Vozár, J. Jančovič, 2012 .

Changes in growth-production parameters of Lolium perenne L. turf after application of concentrated polysulfide fertilizer

P. Kovar, Ľ. Vozár, Peter Hric, 2020 .

Analysis of turf quality in selected headquarters in the district ZLATÉ MORAVCE

P. Kovar, Ľ. Vozár, Peter Hric, 2017 .

Structure-Based Design of A-1293102, a Potent and Selective BCL-XL Inhibitor.

Chaohong Sun, Z. Tao, P. Kovar, 2021, ACS medicinal chemistry letters.

Second-generation peptidomimetic inhibitors of protein farnesyltransferase demonstrating improved cellular potency and significant in vivo efficacy.

S. Ng, P. Kovar, S. Rosenberg, 1999, Journal of medicinal chemistry.

Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor

Xiaohong Song, Z. Tao, P. Kovar, 2020, ACS medicinal chemistry letters.

Methylpyrrole inhibitors of BET bromodomains.

A. Petros, Chaohong Sun, N. Soni, 2017, Bioorganic & medicinal chemistry letters.

Balancing Properties with Carboxylates: A Lead Optimization Campaign for Selective and Orally Active CDK9 Inhibitors.

K. Longenecker, T. Penning, Y. Tong, 2021, ACS medicinal chemistry letters.

Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases.

Scott A. Erickson, S. Davidsen, Eric F. Johnson, 2009, Bioorganic & medicinal chemistry letters.

Growth-Production Parameters of the First Slovak Cultivar of Festulolium A. et Gr.

P. Kovar, Ľ. Vozár, P. Hric, 2018, Acta Universitatis Agriculturae et Silviculturae Mendelianae Brunensis.

Selected qualitative parameters above-ground phytomass of the Lenor-first Slovak cultivar of Festulolium A. et Gr.

P. Kovar, Ľ. Vozár, P. Hric, 2019, Acta fytotechnica et zootechnica.

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.

A. Petros, P. Kovar, Chang H. Park, 2017, Journal of medicinal chemistry.

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.

Ana L. Aguirre, A. Bogdan, Justin D Dietrich, 2018, Bioorganic & medicinal chemistry letters.

Methylpyrrole inhibitors of BET bromodomains.

A. Petros, N. Soni, P. Kovar, 2017, Bioorganic & medicinal chemistry letters.