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Items: 46

1.

Highlights of C (sp2 )-H hydrogen isotope Exchange Reactions.

Hesk D.

J Labelled Comp Radiopharm. 2019 Aug 13. doi: 10.1002/jlcr.3801. [Epub ahead of print]

PMID:
31410875
2.

Deuterated active pharmaceutical ingredients: A science-based proposal for synthesis, analysis, and control. Part 1: Framing the problem.

Czeskis B, Elmore CS, Haight A, Hesk D, Maxwell BD, Miller SA, Raglione T, Schildknegt K, Traverse JF, Wang P.

J Labelled Comp Radiopharm. 2019 Apr 29. doi: 10.1002/jlcr.3743. [Epub ahead of print]

PMID:
31034626
3.

Molecular Interactions in Posaconazole Amorphous Solid Dispersions from Two-Dimensional Solid-State NMR Spectroscopy.

Lu X, Huang C, Lowinger MB, Yang F, Xu W, Brown CD, Hesk D, Koynov A, Schenck L, Su Y.

Mol Pharm. 2019 Jun 3;16(6):2579-2589. doi: 10.1021/acs.molpharmaceut.9b00174. Epub 2019 May 9.

PMID:
31021639
4.

Ni(I)-X Complexes Bearing a Bulky α-Diimine Ligand: Synthesis, Structure, and Superior Catalytic Performance in the Hydrogen Isotope Exchange in Pharmaceuticals.

Zarate C, Yang H, Bezdek MJ, Hesk D, Chirik PJ.

J Am Chem Soc. 2019 Mar 27;141(12):5034-5044. doi: 10.1021/jacs.9b00939. Epub 2019 Mar 13.

PMID:
30827090
5.

MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.

Boga SB, Deng Y, Zhu L, Nan Y, Cooper AB, Shipps GW Jr, Doll R, Shih NY, Zhu H, Sun R, Wang T, Paliwal S, Tsui HC, Gao X, Yao X, Desai J, Wang J, Alhassan AB, Kelly J, Patel M, Muppalla K, Gudipati S, Zhang LK, Buevich A, Hesk D, Carr D, Dayananth P, Black S, Mei H, Cox K, Sherborne B, Hruza AW, Xiao L, Jin W, Long B, Liu G, Taylor SA, Kirschmeier P, Windsor WT, Bishop R, Samatar AA.

ACS Med Chem Lett. 2018 Jun 14;9(7):761-767. doi: 10.1021/acsmedchemlett.8b00220. eCollection 2018 Jul 12.

6.

Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology.

Boga SB, Alhassan AB, Cooper AB, Doll R, Shih NY, Shipps G, Deng Y, Zhu H, Nan Y, Sun R, Zhu L, Desai J, Patel M, Muppalla K, Gao X, Wang J, Yao X, Kelly J, Gudipati S, Paliwal S, Tsui HC, Wang T, Sherborne B, Xiao L, Hruza A, Buevich A, Zhang LK, Hesk D, Samatar AA, Carr D, Long B, Black S, Dayananth P, Windsor W, Kirschmeier P, Bishop R.

Bioorg Med Chem Lett. 2018 Jun 15;28(11):2029-2034. doi: 10.1016/j.bmcl.2018.04.063. Epub 2018 Apr 26.

PMID:
29748051
7.

34 S: A New Opportunity for the Efficient Synthesis of Stable Isotope Labeled Compounds.

Ren S, Fier PS, Ren H, Hoover AJ, Hesk D, Marques R, Mergelsberg I.

Chemistry. 2018 May 17;24(28):7133-7136. doi: 10.1002/chem.201801494. Epub 2018 Apr 26.

PMID:
29604145
8.

Synthesis of 3 H, 13 C2 , 2 H414 C-SCH 430765 and 35 S-SCH 500946, potent and selective inhibitors of the NPY5 receptor.

Hesk D, Koharski D, McNamara P, Royster P, Saluja S, Truong V, Voronin K.

J Labelled Comp Radiopharm. 2018 Jun 15;61(7):533-539. doi: 10.1002/jlcr.3617. Epub 2018 Apr 15.

PMID:
29493011
9.

A General Strategy for Site-Selective Incorporation of Deuterium and Tritium into Pyridines, Diazines, and Pharmaceuticals.

Koniarczyk JL, Hesk D, Overgard A, Davies IW, McNally A.

J Am Chem Soc. 2018 Feb 14;140(6):1990-1993. doi: 10.1021/jacs.7b11710. Epub 2018 Feb 5.

PMID:
29377684
10.

Photoredox-catalyzed deuteration and tritiation of pharmaceutical compounds.

Loh YY, Nagao K, Hoover AJ, Hesk D, Rivera NR, Colletti SL, Davies IW, MacMillan DWC.

Science. 2017 Dec 1;358(6367):1182-1187. doi: 10.1126/science.aap9674. Epub 2017 Nov 9.

11.

Synthesis of 3 H, 2 H4 , and 14 C-MK 3814 (preladenant).

Hesk D, Borges S, Dumpit R, Hendershot S, Koharski D, McNamara P, Ren S, Saluja S, Truong V, Voronin K.

J Labelled Comp Radiopharm. 2017 Apr;60(4):194-199. doi: 10.1002/jlcr.3490. Epub 2017 Mar 17.

PMID:
28129428
12.

Quantitation of wall teichoic acid in Staphylococcus aureus by direct measurement of monomeric units using LC-MS/MS.

Berejnaia O, Wang H, Labroli M, Yang C, Gill C, Xiao J, Hesk D, DeJesus R, Su J, Tan CM, Sheth PR, Kavana M, McLaren DG.

Anal Biochem. 2017 Feb 1;518:9-15. doi: 10.1016/j.ab.2016.10.027. Epub 2016 Nov 2.

PMID:
27815077
13.

IIS 2015 Princeton Conference.

Hesk D, Lavey C, Soli E.

J Labelled Comp Radiopharm. 2016 Dec;59(14):594-600. doi: 10.1002/jlcr.3444. Epub 2016 Oct 2. No abstract available.

PMID:
27696492
14.

Twelfth International Isotope Symposium on the Synthesis and Applications of Isotopes and Isotopically Labelled Compounds (IIS2015).

Hesk D, Lavey C, Soli E.

J Labelled Comp Radiopharm. 2016 Dec;59(14):592-593. doi: 10.1002/jlcr.3438. Epub 2016 Sep 13. No abstract available.

PMID:
27619471
15.

Synthesis of [(14) C]omarigliptin.

Ren S, Gauthier D, Marques R, Helmy R, Hesk D.

J Labelled Comp Radiopharm. 2016 Aug;59(10):386-90. doi: 10.1002/jlcr.3421. Epub 2016 Jun 23.

PMID:
27334864
16.

Preclinical Characterization of 18F-MK-6240, a Promising PET Tracer for In Vivo Quantification of Human Neurofibrillary Tangles.

Hostetler ED, Walji AM, Zeng Z, Miller P, Bennacef I, Salinas C, Connolly B, Gantert L, Haley H, Holahan M, Purcell M, Riffel K, Lohith TG, Coleman P, Soriano A, Ogawa A, Xu S, Zhang X, Joshi E, Della Rocca J, Hesk D, Schenk DJ, Evelhoch JL.

J Nucl Med. 2016 Oct;57(10):1599-1606. Epub 2016 May 26.

17.

Discovery of 6-(Fluoro-(18)F)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine ([(18)F]-MK-6240): A Positron Emission Tomography (PET) Imaging Agent for Quantification of Neurofibrillary Tangles (NFTs).

Walji AM, Hostetler ED, Selnick H, Zeng Z, Miller P, Bennacef I, Salinas C, Connolly B, Gantert L, Holahan M, O'Malley S, Purcell M, Riffel K, Li J, Balsells J, OBrien JA, Melquist S, Soriano A, Zhang X, Ogawa A, Xu S, Joshi E, Della Rocca J, Hess FJ, Schachter J, Hesk D, Schenk D, Struyk A, Babaoglu K, Lohith TG, Wang Y, Yang K, Fu J, Evelhoch JL, Coleman PJ.

J Med Chem. 2016 May 26;59(10):4778-89. doi: 10.1021/acs.jmedchem.6b00166. Epub 2016 May 5.

PMID:
27088900
18.

Synthesis of (3) H, (2) H4 and (14) C-SCH 417690 (Vicriviroc).

Hesk D, Borges S, Hendershot S, Koharski D, McNamara P, Ren S, Saluja S, Truong V, Voronin K.

J Labelled Comp Radiopharm. 2016 May 15;59(5):190-6. doi: 10.1002/jlcr.3387. Epub 2016 Mar 14.

PMID:
26991320
19.

Determining the isotopic abundance of a labeled compound by mass spectrometry and how correcting for natural abundance distribution using analogous data from the unlabeled compound leads to a systematic error.

Schenk DJ, Lockley WJ, Elmore CS, Hesk D, Roberts D.

J Labelled Comp Radiopharm. 2016 Apr;59(4):136-46. doi: 10.1002/jlcr.3370. Epub 2016 Feb 24.

PMID:
26916110
20.

Iron-catalysed tritiation of pharmaceuticals.

Yu RP, Hesk D, Rivera N, Pelczer I, Chirik PJ.

Nature. 2016 Jan 14;529(7585):195-9. doi: 10.1038/nature16464.

PMID:
26762456
21.

In vitro pharmacological characterization of vorapaxar, a novel platelet thrombin receptor antagonist.

Hawes BE, Zhai Y, Hesk D, Wirth M, Wei H, Chintala M, Seiffert D.

Eur J Pharmacol. 2015 Sep 5;762:221-8. doi: 10.1016/j.ejphar.2015.05.046. Epub 2015 May 27.

PMID:
26022529
22.

NMR-based approach to the analysis of radiopharmaceuticals: radiochemical purity, specific activity, and radioactive concentration values by proton and tritium NMR spectroscopy.

Schenk DJ, Dormer PG, Hesk D, Pollack SR, Lavey CF.

J Labelled Comp Radiopharm. 2015 Jun 15;58(7):291-8. doi: 10.1002/jlcr.3295. Epub 2015 May 26.

PMID:
26014438
23.

Synthesis of 3H, 13C,2H3,15N and 14C-labelled SCH 466036, a histamine 3 receptor antagonist.

Hesk D, Borges S, Dumpit R, Hendershot S, Koharski D, Lavey C, McNamara P, Voronin K.

J Labelled Comp Radiopharm. 2015 Feb;58(2):36-41. doi: 10.1002/jlcr.3261.

PMID:
25689968
24.

Synthesis of a [(14) C]-steroid intermediate: an application of a nonstabilized Horner-Wadsworth-Emmons olefination approach.

Rivera NR, Ren S, Hesk D.

J Labelled Comp Radiopharm. 2015 Jan;58(1):20-2. doi: 10.1002/jlcr.3257.

PMID:
25616231
25.

Synthesis of [(3) H], [(13) C3 , (15) N], and [(14) C]SCH 900567: an inhibitor of TNF-α (tumor necrosis factor alpha) converting enzyme (TACE).

Ren S, Hesk D, McNamara P, Koharski D, Borges S.

J Labelled Comp Radiopharm. 2014 Sep;57(11):632-6. doi: 10.1002/jlcr.3229. Epub 2014 Sep 23.

PMID:
25251383
26.

Syntheses of (3) H-labeled, (14) C-labeled, and (2) H4 -labeled SCH 444877, phosphodiesterase type 5 inhibitors.

Ren S, Hesk D, McNamara P, Koharski D, Hendershot S.

J Labelled Comp Radiopharm. 2013 Jul-Aug;56(9-10):480-4. doi: 10.1002/jlcr.3080. Epub 2013 Aug 24.

PMID:
24285525
27.

Discovery of an irreversible HCV NS5B polymerase inhibitor.

Zeng Q, Nair AG, Rosenblum SB, Huang HC, Lesburg CA, Jiang Y, Selyutin O, Chan TY, Bennett F, Chen KX, Venkatraman S, Sannigrahi M, Velazquez F, Duca JS, Gavalas S, Huang Y, Pu H, Wang L, Pinto P, Vibulbhan B, Agrawal S, Ferrari E, Jiang CK, Li C, Hesk D, Gesell J, Sorota S, Shih NY, Njoroge FG, Kozlowski JA.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6585-7. doi: 10.1016/j.bmcl.2013.10.060. Epub 2013 Nov 6.

PMID:
24252545
28.

Precision and accuracy in the quantitative analysis of biological samples by accelerator mass spectrometry: application in microdose absolute bioavailability studies.

Gao L, Li J, Kasserra C, Song Q, Arjomand A, Hesk D, Chowdhury SK.

Anal Chem. 2011 Jul 15;83(14):5607-16. doi: 10.1021/ac2006284. Epub 2011 Jun 20.

PMID:
21627104
29.

SCH529074, a small molecule activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquitination of wild type p53.

Demma M, Maxwell E, Ramos R, Liang L, Li C, Hesk D, Rossman R, Mallams A, Doll R, Liu M, Seidel-Dugan C, Bishop WR, Dasmahapatra B.

J Biol Chem. 2010 Apr 2;285(14):10198-212. doi: 10.1074/jbc.M109.083469. Epub 2010 Feb 2.

30.

Estimation of the extent of oral absorption in animals from oral and intravenous pharmacokinetic data in drug discovery.

Nomeir AA, Morrison R, Prelusky D, Korfmacher W, Broske L, Hesk D, McNamara P, Mei H.

J Pharm Sci. 2009 Nov;98(11):4027-38. doi: 10.1002/jps.21705.

PMID:
19226636
31.

Identification and characterization of pseudoirreversible nonpeptide antagonists of the neuropeptide Y Y5 receptor and development of a novel Y5-selective radioligand.

Mullins D, Adham N, Hesk D, Wu Y, Kelly J, Huang Y, Guzzi M, Zhang X, McCombie S, Stamford A, Parker E.

Eur J Pharmacol. 2008 Dec 28;601(1-3):1-7. doi: 10.1016/j.ejphar.2008.10.021. Epub 2008 Oct 18.

PMID:
18976648
32.

Heterotricyclic himbacine analogs as potent, orally active thrombin receptor (protease activated receptor-1) antagonists.

Chelliah MV, Chackalamannil S, Xia Y, Eagen K, Clasby MC, Gao X, Greenlee W, Ahn HS, Agans-Fantuzzi J, Boykow G, Hsieh Y, Bryant M, Palamanda J, Chan TM, Hesk D, Chintala M.

J Med Chem. 2007 Oct 18;50(21):5147-60. Epub 2007 Sep 14.

PMID:
17854166
33.

Pharmacological characterization of Sch527123, a potent allosteric CXCR1/CXCR2 antagonist.

Gonsiorek W, Fan X, Hesk D, Fossetta J, Qiu H, Jakway J, Billah M, Dwyer M, Chao J, Deno G, Taveras A, Lundell DJ, Hipkin RW.

J Pharmacol Exp Ther. 2007 Aug;322(2):477-85. Epub 2007 May 11.

PMID:
17496166
34.

Characterization of peripheral human cannabinoid receptor (hCB2) expression and pharmacology using a novel radioligand, [35S]Sch225336.

Gonsiorek W, Hesk D, Chen SC, Kinsley D, Fine JS, Jackson JV, Bober LA, Deno G, Bian H, Fossetta J, Lunn CA, Kozlowski JA, Lavey B, Piwinski J, Narula SK, Lundell DJ, Hipkin RW.

J Biol Chem. 2006 Sep 22;281(38):28143-51. Epub 2006 Jun 5.

35.

SCH 503034, a mechanism-based inhibitor of hepatitis C virus NS3 protease, suppresses polyprotein maturation and enhances the antiviral activity of alpha interferon in replicon cells.

Malcolm BA, Liu R, Lahser F, Agrawal S, Belanger B, Butkiewicz N, Chase R, Gheyas F, Hart A, Hesk D, Ingravallo P, Jiang C, Kong R, Lu J, Pichardo J, Prongay A, Skelton A, Tong X, Venkatraman S, Xia E, Girijavallabhan V, Njoroge FG.

Antimicrob Agents Chemother. 2006 Mar;50(3):1013-20.

36.

Identification of full, partial and inverse CC chemokine receptor 3 agonists using [35S]GTPgammaS binding.

Wan Y, Jakway JP, Qiu H, Shah H, Garlisi CG, Tian F, Ting P, Hesk D, Egan RW, Billah MM, Umland SP.

Eur J Pharmacol. 2002 Dec 5;456(1-3):1-10.

PMID:
12450563
37.

Biochemical characterization of desloratadine, a potent antagonist of the human histamine H(1) receptor.

Anthes JC, Gilchrest H, Richard C, Eckel S, Hesk D, West RE Jr, Williams SM, Greenfeder S, Billah M, Kreutner W, Egan RE.

Eur J Pharmacol. 2002 Aug 9;449(3):229-37.

PMID:
12167464
38.

Evernimicin binds exclusively to the 50S ribosomal subunit and inhibits translation in cell-free systems derived from both gram-positive and gram-negative bacteria.

McNicholas PM, Najarian DJ, Mann PA, Hesk D, Hare RS, Shaw KJ, Black TA.

Antimicrob Agents Chemother. 2000 May;44(5):1121-6.

39.

Binding of a thrombin receptor tethered ligand analogue to human platelet thrombin receptor.

Ahn HS, Foster C, Boykow G, Arik L, Smith-Torhan A, Hesk D, Chatterjee M.

Mol Pharmacol. 1997 Feb;51(2):350-6.

PMID:
9203642
40.

Comparison of anacardic acid biosynthetic capability between insect-resistant and-susceptible geraniums.

Hesk D, Craig R, Mumma RO.

J Chem Ecol. 1992 Aug;18(8):1349-64. doi: 10.1007/BF00994361.

PMID:
24254211
41.

A rapid method for isolating glandular trichomes.

Yerger EH, Grazzini RA, Hesk D, Cox-Foster DL, Craig R, Mumma RO.

Plant Physiol. 1992 May;99(1):1-7.

42.
43.

Inhibition of lipoxygenase and prostaglandin endoperoxide synthase by anacardic acids.

Grazzini R, Hesk D, Heininger E, Hildenbrandt G, Reddy CC, Cox-Foster D, Medford J, Craig R, Mumma RO.

Biochem Biophys Res Commun. 1991 Apr 30;176(2):775-80.

PMID:
1902673
44.
45.

The fate of 4-cyanoacetanilide in rats and mice: the mechanism of formation of a novel electrophilic metabolite.

Logan CJ, Hesk D, Hutson DH.

Adv Exp Med Biol. 1986;197:749-53. No abstract available.

PMID:
3766292
46.

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