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Items: 31

1.

High-Throughput Ligand Screening Enables the Enantioselective Conjugate Borylation of Cyclobutenones to Access Synthetically Versatile Tertiary Cyclobutylboronates.

Clement HA, Boghi M, McDonald RM, Bernier L, Coe JW, Farrell W, Helal CJ, Reese MR, Sach NW, Lee JC, Hall DG.

Angew Chem Int Ed Engl. 2019 Dec 16;58(51):18405-18409. doi: 10.1002/anie.201909308. Epub 2019 Oct 31.

PMID:
31591755
2.

Quick Building Blocks (QBB): An Innovative and Efficient Business Model To Speed Medicinal Chemistry Analog Synthesis.

Helal CJ, Bundesmann M, Hammond S, Holmstrom M, Klug-McLeod J, Lefker BA, McLeod D, Subramanyam C, Zakaryants O, Sakata S.

ACS Med Chem Lett. 2019 Jul 5;10(8):1104-1109. doi: 10.1021/acsmedchemlett.9b00205. eCollection 2019 Aug 8.

PMID:
31413793
3.

Synthetic Approaches to the New Drugs Approved During 2017.

Flick AC, Leverett CA, Ding HX, McInturff E, Fink SJ, Helal CJ, O'Donnell CJ.

J Med Chem. 2019 Aug 22;62(16):7340-7382. doi: 10.1021/acs.jmedchem.9b00196. Epub 2019 Apr 15.

PMID:
30939001
4.

Correction to Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.

Helal CJ, Arnold EP, Boyden TL, Chang C, Chappie TA, Fennell KF, Forman MD, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Kang Z, Kleiman RJ, Kormos BL, LaChapelle EA, Lee CW, Lu J, Maklad N, McDowell L, Mente S, O'Connor RE, Pandit J, Piotrowski M, Schmidt AW, Schmidt CJ, Ueno H, Verhoest PR, Yang EX.

J Med Chem. 2018 Apr 26;61(8):3753. doi: 10.1021/acs.jmedchem.8b00475. Epub 2018 Apr 6. No abstract available.

PMID:
29624389
5.

Increased building block access through collaboration.

Helal CJ, Bartolozzi A, Goble SD, Mani NS, Guzman-Perez A, Ohri AK, Shi ZC, Subramanyam C.

Drug Discov Today. 2018 Aug;23(8):1458-1462. doi: 10.1016/j.drudis.2018.03.001. Epub 2018 Mar 20. Review. No abstract available.

PMID:
29571837
6.

Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation.

McAllister LA, Butler CR, Mente S, O'Neil SV, Fonseca KR, Piro JR, Cianfrogna JA, Foley TL, Gilbert AM, Harris AR, Helal CJ, Johnson DS, Montgomery JI, Nason DM, Noell S, Pandit J, Rogers BN, Samad TA, Shaffer CL, da Silva RG, Uccello DP, Webb D, Brodney MA.

J Med Chem. 2018 Apr 12;61(7):3008-3026. doi: 10.1021/acs.jmedchem.8b00070. Epub 2018 Mar 15.

PMID:
29498843
7.

Late-Stage Microsomal Oxidation Reduces Drug-Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189.

Stepan AF, Tran TP, Helal CJ, Brown MS, Chang C, O'Connor RE, De Vivo M, Doran SD, Fisher EL, Jenkinson S, Karanian D, Kormos BL, Sharma R, Walker GS, Wright AS, Yang EX, Brodney MA, Wager TT, Verhoest PR, Obach RS.

ACS Med Chem Lett. 2018 Jan 4;9(2):68-72. doi: 10.1021/acsmedchemlett.7b00343. eCollection 2018 Feb 8.

8.

A platform for automated nanomole-scale reaction screening and micromole-scale synthesis in flow.

Perera D, Tucker JW, Brahmbhatt S, Helal CJ, Chong A, Farrell W, Richardson P, Sach NW.

Science. 2018 Jan 26;359(6374):429-434. doi: 10.1126/science.aap9112.

PMID:
29371464
9.

Introduction of a Crystalline, Shelf-Stable Reagent for the Synthesis of Sulfur(VI) Fluorides.

Zhou H, Mukherjee P, Liu R, Evrard E, Wang D, Humphrey JM, Butler TW, Hoth LR, Sperry JB, Sakata SK, Helal CJ, Am Ende CW.

Org Lett. 2018 Feb 2;20(3):812-815. doi: 10.1021/acs.orglett.7b03950. Epub 2018 Jan 12.

PMID:
29327935
10.

Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.

Helal CJ, Arnold E, Boyden T, Chang C, Chappie TA, Fisher E, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Pandit J, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, McGinnis D, O'Connor RE, O'Donnell CJ, Ogden A, Piotrowski M, Schmidt CJ, Seymour PA, Ueno H, Vansell N, Verhoest PR, Yang EX.

J Med Chem. 2018 Feb 8;61(3):1001-1018. doi: 10.1021/acs.jmedchem.7b01466. Epub 2018 Jan 16.

PMID:
29293004
11.

Parallel Synthesis of 1H-Pyrazolo[3,4-d]pyrimidines via Condensation of N-Pyrazolylamides and Nitriles.

Shah AA, Chenard LK, Tucker JW, Helal CJ.

ACS Comb Sci. 2017 Nov 13;19(11):675-680. doi: 10.1021/acscombsci.7b00116. Epub 2017 Oct 20.

PMID:
28985050
12.

The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging.

Zhang L, Chen L, Beck EM, Chappie TA, Coelho RV, Doran SD, Fan KH, Helal CJ, Humphrey JM, Hughes Z, Kuszpit K, Lachapelle EA, Lazzaro JT, Lee C, Mather RJ, Patel NC, Skaddan MB, Sciabola S, Verhoest PR, Young JM, Zasadny K, Villalobos A.

J Med Chem. 2017 Oct 26;60(20):8538-8551. doi: 10.1021/acs.jmedchem.7b01050. Epub 2017 Oct 9.

PMID:
28957634
13.

Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.

Helal CJ, Arnold EP, Boyden TL, Chang C, Chappie TA, Fennell KF, Forman MD, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, Mente S, O'Connor RE, Pandit J, Piotrowski M, Schmidt AW, Schmidt CJ, Ueno H, Verhoest PR, Yang EX.

J Med Chem. 2017 Jul 13;60(13):5673-5698. doi: 10.1021/acs.jmedchem.7b00397. Epub 2017 Jun 16. Erratum in: J Med Chem. 2018 Apr 26;61(8):3753.

PMID:
28574706
14.

Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.

Butler CR, Ogilvie K, Martinez-Alsina L, Barreiro G, Beck EM, Nolan CE, Atchison K, Benvenuti E, Buzon L, Doran S, Gonzales C, Helal CJ, Hou X, Hsu MH, Johnson EF, Lapham K, Lanyon L, Parris K, O'Neill BT, Riddell D, Robshaw A, Vajdos F, Brodney MA.

J Med Chem. 2017 Jan 12;60(1):386-402. doi: 10.1021/acs.jmedchem.6b01451. Epub 2016 Dec 20.

15.

Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.

Pettersson M, Johnson DS, Rankic DA, Kauffman GW, Am Ende CW, Butler TW, Boscoe B, Evrard E, Helal CJ, Humphrey JM, Stepan AF, Stiff CM, Yang E, Xie L, Bales KR, Hajos-Korcsok E, Jenkinson S, Pettersen B, Pustilnik LR, Ramirez DS, Steyn SJ, Wood KM, Verhoest PR.

Medchemcomm. 2016 Nov 2;8(4):730-743. doi: 10.1039/c6md00406g. eCollection 2017 Apr 1.

16.

Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects.

Davoren JE, Lee CW, Garnsey M, Brodney MA, Cordes J, Dlugolenski K, Edgerton JR, Harris AR, Helal CJ, Jenkinson S, Kauffman GW, Kenakin TP, Lazzaro JT, Lotarski SM, Mao Y, Nason DM, Northcott C, Nottebaum L, O'Neil SV, Pettersen B, Popiolek M, Reinhart V, Salomon-Ferrer R, Steyn SJ, Webb D, Zhang L, Grimwood S.

J Med Chem. 2016 Jul 14;59(13):6313-28. doi: 10.1021/acs.jmedchem.6b00544. Epub 2016 Jul 1.

PMID:
27275946
17.

Preclinical Evaluation of 18F-PF-05270430, a Novel PET Radioligand for the Phosphodiesterase 2A Enzyme.

Chen L, Nabulsi N, Naganawa M, Zasadny K, Skaddan MB, Zhang L, Najafzadeh S, Lin SF, Helal CJ, Boyden TL, Chang C, Ropchan J, Carson RE, Villalobos A, Huang Y.

J Nucl Med. 2016 Sep;57(9):1448-53. doi: 10.2967/jnumed.115.171454. Epub 2016 May 19.

18.

Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design.

Butler CR, Brodney MA, Beck EM, Barreiro G, Nolan CE, Pan F, Vajdos F, Parris K, Varghese AH, Helal CJ, Lira R, Doran SD, Riddell DR, Buzon LM, Dutra JK, Martinez-Alsina LA, Ogilvie K, Murray JC, Young JM, Atchison K, Robshaw A, Gonzales C, Wang J, Zhang Y, O'Neill BT.

J Med Chem. 2015 Mar 26;58(6):2678-702. doi: 10.1021/jm501833t. Epub 2015 Mar 9.

PMID:
25695670
19.

Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development of a novel phosphodiesterase 2A PET ligand.

Zhang L, Villalobos A, Beck EM, Bocan T, Chappie TA, Chen L, Grimwood S, Heck SD, Helal CJ, Hou X, Humphrey JM, Lu J, Skaddan MB, McCarthy TJ, Verhoest PR, Wager TT, Zasadny K.

J Med Chem. 2013 Jun 13;56(11):4568-79. doi: 10.1021/jm400312y. Epub 2013 May 28.

PMID:
23651455
20.

Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors.

Claffey MM, Helal CJ, Verhoest PR, Kang Z, Fors KS, Jung S, Zhong J, Bundesmann MW, Hou X, Lui S, Kleiman RJ, Vanase-Frawley M, Schmidt AW, Menniti F, Schmidt CJ, Hoffman WE, Hajos M, McDowell L, O'Connor RE, Macdougall-Murphy M, Fonseca KR, Becker SL, Nelson FR, Liras S.

J Med Chem. 2012 Nov 8;55(21):9055-68. doi: 10.1021/jm3009635. Epub 2012 Oct 12.

PMID:
23025719
21.

Current landscape of phosphodiesterase 10A (PDE10A) inhibition.

Chappie TA, Helal CJ, Hou X.

J Med Chem. 2012 Sep 13;55(17):7299-331. doi: 10.1021/jm3004976. Epub 2012 Aug 14. No abstract available.

PMID:
22834877
22.

Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders.

Verhoest PR, Fonseca KR, Hou X, Proulx-Lafrance C, Corman M, Helal CJ, Claffey MM, Tuttle JB, Coffman KJ, Liu S, Nelson F, Kleiman RJ, Menniti FS, Schmidt CJ, Vanase-Frawley M, Liras S.

J Med Chem. 2012 Nov 8;55(21):9045-54. doi: 10.1021/jm3007799. Epub 2012 Jul 25.

PMID:
22780914
23.

Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus CYP3A5 in the metabolism of drugs.

Walsky RL, Obach RS, Hyland R, Kang P, Zhou S, West M, Geoghegan KF, Helal CJ, Walker GS, Goosen TC, Zientek MA.

Drug Metab Dispos. 2012 Sep;40(9):1686-97. doi: 10.1124/dmd.112.045302. Epub 2012 May 29.

PMID:
22645092
24.

Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo.

Kleiman RJ, Chapin DS, Christoffersen C, Freeman J, Fonseca KR, Geoghegan KF, Grimwood S, Guanowsky V, Hajós M, Harms JF, Helal CJ, Hoffmann WE, Kocan GP, Majchrzak MJ, McGinnis D, McLean S, Menniti FS, Nelson F, Roof R, Schmidt AW, Seymour PA, Stephenson DT, Tingley FD, Vanase-Frawley M, Verhoest PR, Schmidt CJ.

J Pharmacol Exp Ther. 2012 May;341(2):396-409. doi: 10.1124/jpet.111.191353. Epub 2012 Feb 10.

PMID:
22328573
25.

Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia.

Helal CJ, Kang Z, Hou X, Pandit J, Chappie TA, Humphrey JM, Marr ES, Fennell KF, Chenard LK, Fox C, Schmidt CJ, Williams RD, Chapin DS, Siuciak J, Lebel L, Menniti F, Cianfrogna J, Fonseca KR, Nelson FR, O'Connor R, MacDougall M, McDowell L, Liras S.

J Med Chem. 2011 Jul 14;54(13):4536-47. doi: 10.1021/jm2001508. Epub 2011 Jun 8.

PMID:
21650160
26.

Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.

Verhoest PR, Proulx-Lafrance C, Corman M, Chenard L, Helal CJ, Hou X, Kleiman R, Liu S, Marr E, Menniti FS, Schmidt CJ, Vanase-Frawley M, Schmidt AW, Williams RD, Nelson FR, Fonseca KR, Liras S.

J Med Chem. 2009 Dec 24;52(24):7946-9. doi: 10.1021/jm9015334.

PMID:
19919087
27.

Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's disease.

Helal CJ, Kang Z, Lucas JC, Gant T, Ahlijanian MK, Schachter JB, Richter KE, Cook JM, Menniti FS, Kelly K, Mente S, Pandit J, Hosea N.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5703-7. doi: 10.1016/j.bmcl.2009.08.019. Epub 2009 Aug 8.

PMID:
19700321
28.

Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.

Helal CJ, Sanner MA, Cooper CB, Gant T, Adam M, Lucas JC, Kang Z, Kupchinsky S, Ahlijanian MK, Tate B, Menniti FS, Kelly K, Peterson M.

Bioorg Med Chem Lett. 2004 Nov 15;14(22):5521-5.

PMID:
15482916
29.

Stereoselective synthesis of cis-1,3-disubstituted cyclobutyl kinase inhibitors.

Helal CJ, Kang Z, Lucas JC, Bohall BR.

Org Lett. 2004 May 27;6(11):1853-6. Erratum in: Org Lett. 2004 Aug 19;6(17):3017.

PMID:
15151431
30.

A concise and regioselective synthesis of 1-alkyl-4-imidazolecarboxylates.

Helal CJ, Lucas JC.

Org Lett. 2002 Nov 14;4(23):4133-4.

PMID:
12423104
31.

Reduction of Carbonyl Compounds with Chiral Oxazaborolidine Catalysts: A New Paradigm for Enantioselective Catalysis and a Powerful New Synthetic Method.

Corey EJ, Helal CJ.

Angew Chem Int Ed Engl. 1998 Aug 17;37(15):1986-2012. doi: 10.1002/(SICI)1521-3773(19980817)37:15<1986::AID-ANIE1986>3.0.CO;2-Z. Review.

PMID:
29711061

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