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Items: 28


LRRK2 activation in idiopathic Parkinson's disease.

Di Maio R, Hoffman EK, Rocha EM, Keeney MT, Sanders LH, De Miranda BR, Zharikov A, Van Laar A, Stepan AF, Lanz TA, Kofler JK, Burton EA, Alessi DR, Hastings TG, Greenamyre JT.

Sci Transl Med. 2018 Jul 25;10(451). pii: eaar5429. doi: 10.1126/scitranslmed.aar5429.


Synthesis and applications of highly functionalized 1-halo-3-substituted bicyclo[1.1.1]pentanes.

Caputo DFJ, Arroniz C, Dürr AB, Mousseau JJ, Stepan AF, Mansfield SJ, Anderson EA.

Chem Sci. 2018 May 21;9(23):5295-5300. doi: 10.1039/c8sc01355a. eCollection 2018 Jun 21.


Lead Diversification at the Nanomole Scale Using Liver Microsomes and Quantitative Nuclear Magnetic Resonance Spectroscopy: Application to Phosphodiesterase 2 Inhibitors.

Obach RS, Walker GS, Sharma R, Jenkinson S, Tran TP, Stepan AF.

J Med Chem. 2018 Apr 26;61(8):3626-3640. doi: 10.1021/acs.jmedchem.8b00116. Epub 2018 Apr 9.


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.


Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates.

Stepan AF, Claffey MM, Reese MR, Balan G, Barreiro G, Barricklow J, Bohanon MJ, Boscoe BP, Cappon GD, Chenard LK, Cianfrogna J, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Ghosh S, Hou X, Houle C, Karki K, Lazzaro JT, Mancuso JY, Marcek JM, Miller EL, Moen MA, O'Neil S, Sakurada I, Skaddan M, Parikh V, Smith DL, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Won A, Wright AS, Whritenour J, Zasadny K, Zaleska MM, Zhang L, Shaffer CL.

J Med Chem. 2017 Sep 28;60(18):7764-7780. doi: 10.1021/acs.jmedchem.7b00604. Epub 2017 Sep 13.


Mechanisms of Skin Toxicity Associated with Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators.

Shah F, Stepan AF, O'Mahony A, Velichko S, Folias AE, Houle C, Shaffer CL, Marcek J, Whritenour J, Stanton R, Berg EL.

Cell Chem Biol. 2017 Jul 20;24(7):858-869.e5. doi: 10.1016/j.chembiol.2017.06.003. Epub 2017 Jun 29.


A multi-endpoint matched molecular pair (MMP) analysis of 6-membered heterocycles.

Chang G, Huard K, Kauffman GW, Stepan AF, Keefer CE.

Bioorg Med Chem. 2017 Jan 1;25(1):381-388. doi: 10.1016/j.bmc.2016.11.004. Epub 2016 Nov 2.


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.


Oxidative diversification of amino acids and peptides by small-molecule iron catalysis.

Osberger TJ, Rogness DC, Kohrt JT, Stepan AF, White MC.

Nature. 2016 Sep 8;537(7619):214-219. doi: 10.1038/nature18941. Epub 2016 Aug 1.


Synthesis and Biopharmaceutical Evaluation of Imatinib Analogues Featuring Unusual Structural Motifs.

Nicolaou KC, Vourloumis D, Totokotsopoulos S, Papakyriakou A, Karsunky H, Fernando H, Gavrilyuk J, Webb D, Stepan AF.

ChemMedChem. 2016 Jan 5;11(1):31-7. doi: 10.1002/cmdc.201500510. Epub 2015 Nov 20.


Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability.

Pettersson M, Johnson DS, Humphrey JM, Butler TW, Am Ende CW, Fish BA, Green ME, Kauffman GW, Mullins PB, O'Donnell CJ, Stepan AF, Stiff CM, Subramanyam C, Tran TP, Vetelino BC, Yang E, Xie L, Bales KR, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR.

ACS Med Chem Lett. 2015 Apr 3;6(5):596-601. doi: 10.1021/acsmedchemlett.5b00070. eCollection 2015 May 14.


Discovery of indole-derived pyridopyrazine-1,6-dione γ-secretase modulators that target presenilin.

Pettersson M, Johnson DS, Humphrey JM, Am Ende CW, Evrard E, Efremov I, Kauffman GW, Stepan AF, Stiff CM, Xie L, Bales KR, Hajos-Korcsok E, Murrey HE, Pustilnik LR, Steyn SJ, Wood KM, Verhoest PR.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):908-13. doi: 10.1016/j.bmcl.2014.12.059. Epub 2014 Dec 25.


Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.

Zhang L, Balan G, Barreiro G, Boscoe BP, Chenard LK, Cianfrogna J, Claffey MM, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Fonseca KR, Galatsis P, Grimwood S, Lazzaro JT, Mancuso JY, Miller EL, Reese MR, Rogers BN, Sakurada I, Skaddan M, Smith DL, Stepan AF, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Wright AS, Zaleska MM, Zasadny K, Shaffer CL.

J Med Chem. 2014 Feb 13;57(3):861-77. doi: 10.1021/jm401622k. Epub 2014 Jan 22.


Evaluating the differences in cycloalkyl ether metabolism using the design parameter "lipophilic metabolism efficiency" (LipMetE) and a matched molecular pairs analysis.

Stepan AF, Kauffman GW, Keefer CE, Verhoest PR, Edwards M.

J Med Chem. 2013 Sep 12;56(17):6985-90. doi: 10.1021/jm4008642. Epub 2013 Aug 21.


Novel γ-secretase modulators for the treatment of Alzheimer's disease: a review focusing on patents from 2010 to 2012.

Pettersson M, Stepan AF, Kauffman GW, Johnson DS.

Expert Opin Ther Pat. 2013 Oct;23(10):1349-66. doi: 10.1517/13543776.2013.821465. Epub 2013 Jul 23. Review.


Discovery of Dap-3 polymyxin analogues for the treatment of multidrug-resistant Gram-negative nosocomial infections.

Magee TV, Brown MF, Starr JT, Ackley DC, Abramite JA, Aubrecht J, Butler A, Crandon JL, Dib-Hajj F, Flanagan ME, Granskog K, Hardink JR, Huband MD, Irvine R, Kuhn M, Leach KL, Li B, Lin J, Luke DR, MacVane SH, Miller AA, McCurdy S, McKim JM Jr, Nicolau DP, Nguyen TT, Noe MC, O'Donnell JP, Seibel SB, Shen Y, Stepan AF, Tomaras AP, Wilga PC, Zhang L, Xu J, Chen JM.

J Med Chem. 2013 Jun 27;56(12):5079-93. doi: 10.1021/jm400416u. Epub 2013 Jun 18.


Pd(II)-catalyzed ortho- or meta-C-H olefination of phenol derivatives.

Dai HX, Li G, Zhang XG, Stepan AF, Yu JQ.

J Am Chem Soc. 2013 May 22;135(20):7567-71. doi: 10.1021/ja400659s. Epub 2013 May 8.


Application of the bicyclo[1.1.1]pentane motif as a nonclassical phenyl ring bioisostere in the design of a potent and orally active γ-secretase inhibitor.

Stepan AF, Subramanyam C, Efremov IV, Dutra JK, O'Sullivan TJ, DiRico KJ, McDonald WS, Won A, Dorff PH, Nolan CE, Becker SL, Pustilnik LR, Riddell DR, Kauffman GW, Kormos BL, Zhang L, Lu Y, Capetta SH, Green ME, Karki K, Sibley E, Atchison KP, Hallgren AJ, Oborski CE, Robshaw AE, Sneed B, O'Donnell CJ.

J Med Chem. 2012 Apr 12;55(7):3414-24. doi: 10.1021/jm300094u. Epub 2012 Mar 29.


Sequential allylic C-H amination/vinylic C-H arylation: a strategy for unnatural amino acid synthesis from α-olefins.

Jiang C, Covell DJ, Stepan AF, Plummer MS, White MC.

Org Lett. 2012 Mar 16;14(6):1386-9. doi: 10.1021/ol300063t. Epub 2012 Feb 24.


Metabolism-directed design of oxetane-containing arylsulfonamide derivatives as γ-secretase inhibitors.

Stepan AF, Karki K, McDonald WS, Dorff PH, Dutra JK, Dirico KJ, Won A, Subramanyam C, Efremov IV, O'Donnell CJ, Nolan CE, Becker SL, Pustilnik LR, Sneed B, Sun H, Lu Y, Robshaw AE, Riddell D, O'Sullivan TJ, Sibley E, Capetta S, Atchison K, Hallgren AJ, Miller E, Wood A, Obach RS.

J Med Chem. 2011 Nov 24;54(22):7772-83. doi: 10.1021/jm200893p. Epub 2011 Oct 26.


Oxidative metabolism of a quinoxaline derivative by xanthine oxidase in rodent plasma.

Sharma R, Eng H, Walker GS, Barreiro G, Stepan AF, McClure KF, Wolford A, Bonin PD, Cornelius P, Kalgutkar AS.

Chem Res Toxicol. 2011 Dec 19;24(12):2207-16. doi: 10.1021/tx200329k. Epub 2011 Oct 4.


Quantitative pharmacokinetic/pharmacodynamic analyses suggest that the 129/SVE mouse is a suitable preclinical pharmacology model for identifying small-molecule γ-secretase inhibitors.

Lu Y, Zhang L, Nolan CE, Becker SL, Atchison K, Robshaw AE, Pustilnik LR, Osgood SM, Miller EH, Stepan AF, Subramanyam C, Efremov I, Hallgren AJ, Riddell D.

J Pharmacol Exp Ther. 2011 Dec;339(3):922-34. doi: 10.1124/jpet.111.186791. Epub 2011 Sep 19.


Structural alert/reactive metabolite concept as applied in medicinal chemistry to mitigate the risk of idiosyncratic drug toxicity: a perspective based on the critical examination of trends in the top 200 drugs marketed in the United States.

Stepan AF, Walker DP, Bauman J, Price DA, Baillie TA, Kalgutkar AS, Aleo MD.

Chem Res Toxicol. 2011 Sep 19;24(9):1345-410. doi: 10.1021/tx200168d. Epub 2011 Jul 11. Review.


Divergent C-H functionalizations directed by sulfonamide pharmacophores: late-stage diversification as a tool for drug discovery.

Dai HX, Stepan AF, Plummer MS, Zhang YH, Yu JQ.

J Am Chem Soc. 2011 May 11;133(18):7222-8. doi: 10.1021/ja201708f. Epub 2011 Apr 13.


Design, synthesis, and biological evaluation of platensimycin analogues with varying degrees of molecular complexity.

Nicolaou KC, Stepan AF, Lister T, Li A, Montero A, Tria GS, Turner CI, Tang Y, Wang J, Denton RM, Edmonds DJ.

J Am Chem Soc. 2008 Oct 1;130(39):13110-9. doi: 10.1021/ja8044376. Epub 2008 Sep 5.


Total synthesis and antibacterial properties of carbaplatensimycin.

Nicolaou KC, Tang Y, Wang J, Stepan AF, Li A, Montero A.

J Am Chem Soc. 2007 Dec 5;129(48):14850-1. Epub 2007 Nov 8.


Diastereoselective aldol reactions with butane-2,3-diacetal protected glyceraldehyde derivatives.

Knudsen KR, Stepan AF, Michel P, Ley SV.

Org Biomol Chem. 2006 Apr 21;4(8):1471-3. Epub 2006 Mar 13. Erratum in: Org Biomol Chem. 2006 Apr 21;4(8):1612.


Palladium-containing perovskites: recoverable and reuseable catalysts for Suzuki couplings.

Smith MD, Stepan AF, Ramarao C, Brennan PE, Ley SV.

Chem Commun (Camb). 2003 Nov 7;(21):2652-3.


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