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Items: 32

1.

Discovery of potent azaindazole leucine-rich repeat kinase 2 (LRRK2) inhibitors possessing a key intramolecular hydrogen bond - Part 2.

Shore DGM, Sweeney ZK, Beresford A, Chan BK, Chen H, Drummond J, Gill A, Kleinheinz T, Liu X, Medhurst AD, McIver EG, Moffat JG, Zhu H, Estrada AA.

Bioorg Med Chem Lett. 2019 Feb 15;29(4):674-680. doi: 10.1016/j.bmcl.2018.10.017. Epub 2018 Oct 12.

PMID:
30522953
2.

Application of Virtual Screening to the Identification of New LpxC Inhibitor Chemotypes, Oxazolidinone and Isoxazoline.

Lee PS, Lapointe G, Madera AM, Simmons RL, Xu W, Yifru A, Tjandra M, Karur S, Rico A, Thompson K, Bojkovic J, Xie L, Uehara K, Liu A, Shu W, Bellamacina C, McKenney D, Morris L, Tonn GR, Osborne C, Benton BM, McDowell L, Fu J, Sweeney ZK.

J Med Chem. 2018 Oct 25;61(20):9360-9370. doi: 10.1021/acs.jmedchem.8b01287. Epub 2018 Oct 3.

PMID:
30226381
3.

Targeting of nonlipidated, aggregated apoE with antibodies inhibits amyloid accumulation.

Liao F, Li A, Xiong M, Bien-Ly N, Jiang H, Zhang Y, Finn MB, Hoyle R, Keyser J, Lefton KB, Robinson GO, Serrano JR, Silverman AP, Guo JL, Getz J, Henne K, Leyns CE, Gallardo G, Ulrich JD, Sullivan PM, Lerner EP, Hudry E, Sweeney ZK, Dennis MS, Hyman BT, Watts RJ, Holtzman DM.

J Clin Invest. 2018 May 1;128(5):2144-2155. doi: 10.1172/JCI96429. Epub 2018 Mar 30.

4.

Development of a cyclosporin A derivative with excellent anti-hepatitis C virus potency.

Fu J, Becker C, Cao L, Capparelli M, Denay R, Fujimoto R, Gai Y, Gao Z, Guenat C, Karur S, Kim H, Li W, Li X, Li W, Lochmann T, Lu A, Lu P, Luneau A, Meier N, Mergo W, Ng S, Parker D, Peng Y, Riss B, Rivkin A, Roggo S, Schroeder H, Schuerch F, Simmons RL, Sun F, Sweeney ZK, Tjandra M, Wang M, Wang R, Weiss AH, Wenger N, Wu Q, Xiong X, Xu S, Xu W, Yifru A, Zhao J, Zhou J, Zürcher C, Gallou F.

Bioorg Med Chem. 2018 Feb 15;26(4):957-969. doi: 10.1016/j.bmc.2017.09.008. Epub 2017 Sep 7.

PMID:
28919180
5.

Chemical Biology of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors.

Estrada AA, Sweeney ZK.

J Med Chem. 2015 Sep 10;58(17):6733-46. doi: 10.1021/acs.jmedchem.5b00261. Epub 2015 May 14.

PMID:
25915084
6.

Effect of selective LRRK2 kinase inhibition on nonhuman primate lung.

Fuji RN, Flagella M, Baca M, Baptista MA, Brodbeck J, Chan BK, Fiske BK, Honigberg L, Jubb AM, Katavolos P, Lee DW, Lewin-Koh SC, Lin T, Liu X, Liu S, Lyssikatos JP, O'Mahony J, Reichelt M, Roose-Girma M, Sheng Z, Sherer T, Smith A, Solon M, Sweeney ZK, Tarrant J, Urkowitz A, Warming S, Yaylaoglu M, Zhang S, Zhu H, Estrada AA, Watts RJ.

Sci Transl Med. 2015 Feb 4;7(273):273ra15. doi: 10.1126/scitranslmed.aaa3634.

PMID:
25653221
7.

Promiscuity and the conformational rearrangement of drug-like molecules: insight from the protein data bank.

He MW, Lee PS, Sweeney ZK.

ChemMedChem. 2015 Feb;10(2):238-44. doi: 10.1002/cmdc.201402389. Epub 2014 Dec 9.

PMID:
25491400
8.

Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.

Lou Y, Sweeney ZK, Kuglstatter A, Davis D, Goldstein DM, Han X, Hong J, Kocer B, Kondru RK, Litman R, McIntosh J, Sarma K, Suh J, Taygerly J, Owens TD.

Bioorg Med Chem Lett. 2015 Jan 15;25(2):367-71. doi: 10.1016/j.bmcl.2014.11.030. Epub 2014 Nov 20.

PMID:
25466710
9.

Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition.

Fu J, Tjandra M, Becker C, Bednarczyk D, Capparelli M, Elling R, Hanna I, Fujimoto R, Furegati M, Karur S, Kasprzyk T, Knapp M, Leung K, Li X, Lu P, Mergo W, Miault C, Ng S, Parker D, Peng Y, Roggo S, Rivkin A, Simmons RL, Wang M, Wiedmann B, Weiss AH, Xiao L, Xie L, Xu W, Yifru A, Yang S, Zhou B, Sweeney ZK.

J Med Chem. 2014 Oct 23;57(20):8503-16. doi: 10.1021/jm500862r. Epub 2014 Oct 13.

PMID:
25310383
10.

From chemical tools to clinical medicines: nonimmunosuppressive cyclophilin inhibitors derived from the cyclosporin and sanglifehrin scaffolds.

Sweeney ZK, Fu J, Wiedmann B.

J Med Chem. 2014 Sep 11;57(17):7145-59. doi: 10.1021/jm500223x. Epub 2014 Jun 3.

PMID:
24831536
11.

Structure-based drug design of RN486, a potent and selective Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis.

Lou Y, Han X, Kuglstatter A, Kondru RK, Sweeney ZK, Soth M, McIntosh J, Litman R, Suh J, Kocer B, Davis D, Park J, Frauchiger S, Dewdney N, Zecic H, Taygerly JP, Sarma K, Hong J, Hill RJ, Gabriel T, Goldstein DM, Owens TD.

J Med Chem. 2015 Jan 8;58(1):512-6. doi: 10.1021/jm500305p. Epub 2014 Apr 16.

PMID:
24712864
12.

Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

Estrada AA, Chan BK, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chen H, Dominguez SL, Dotson J, Drummond J, Flagella M, Fuji R, Gill A, Halladay J, Harris SF, Heffron TP, Kleinheinz T, Lee DW, Le Pichon CE, Liu X, Lyssikatos JP, Medhurst AD, Moffat JG, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Wong S, Zhang S, Zhang X, Zhu H, Sweeney ZK.

J Med Chem. 2014 Feb 13;57(3):921-36. doi: 10.1021/jm401654j. Epub 2014 Jan 15.

PMID:
24354345
13.

Identification of GNE-293, a potent and selective PI3Kδ inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.

Safina BS, Sweeney ZK, Li J, Chan BK, Bisconte A, Carrera D, Castanedo G, Flagella M, Heald R, Lewis C, Murray JM, Nonomiya J, Pang J, Price S, Reif K, Salphati L, Seward EM, Wei B, Sutherlin DP.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4953-9. doi: 10.1016/j.bmcl.2013.06.052. Epub 2013 Jun 29.

14.

Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor.

Chan BK, Estrada AA, Chen H, Atherall J, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Dominguez SL, Drummond J, Gill A, Kleinheinz T, Le Pichon CE, Medhurst AD, Liu X, Moffat JG, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Van de Poël H, Zhang S, Zhu H, Sweeney ZK.

ACS Med Chem Lett. 2012 Nov 23;4(1):85-90. doi: 10.1021/ml3003007. eCollection 2013 Jan 10.

15.

Ser1292 autophosphorylation is an indicator of LRRK2 kinase activity and contributes to the cellular effects of PD mutations.

Sheng Z, Zhang S, Bustos D, Kleinheinz T, Le Pichon CE, Dominguez SL, Solanoy HO, Drummond J, Zhang X, Ding X, Cai F, Song Q, Li X, Yue Z, van der Brug MP, Burdick DJ, Gunzner-Toste J, Chen H, Liu X, Estrada AA, Sweeney ZK, Scearce-Levie K, Moffat JG, Kirkpatrick DS, Zhu H.

Sci Transl Med. 2012 Dec 12;4(164):164ra161. doi: 10.1126/scitranslmed.3004485.

16.

Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

Estrada AA, Liu X, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chan BK, Chen H, Ding X, DiPasquale AG, Dominguez SL, Dotson J, Drummond J, Flagella M, Flynn S, Fuji R, Gill A, Gunzner-Toste J, Harris SF, Heffron TP, Kleinheinz T, Lee DW, Le Pichon CE, Lyssikatos JP, Medhurst AD, Moffat JG, Mukund S, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Tran T, Trivedi N, Wang S, Zhang S, Zhang X, Zhao G, Zhu H, Sweeney ZK.

J Med Chem. 2012 Nov 26;55(22):9416-33. doi: 10.1021/jm301020q. Epub 2012 Oct 15.

PMID:
22985112
17.

Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.

Murray JM, Sweeney ZK, Chan BK, Balazs M, Bradley E, Castanedo G, Chabot C, Chantry D, Flagella M, Goldstein DM, Kondru R, Lesnick J, Li J, Lucas MC, Nonomiya J, Pang J, Price S, Salphati L, Safina B, Savy PP, Seward EM, Ultsch M, Sutherlin DP.

J Med Chem. 2012 Sep 13;55(17):7686-95. doi: 10.1021/jm300717c. Epub 2012 Aug 21.

PMID:
22877085
18.

Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.

Sutherlin DP, Baker S, Bisconte A, Blaney PM, Brown A, Chan BK, Chantry D, Castanedo G, DePledge P, Goldsmith P, Goldstein DM, Hancox T, Kaur J, Knowles D, Kondru R, Lesnick J, Lucas MC, Lewis C, Murray J, Nadin AJ, Nonomiya J, Pang J, Pegg N, Price S, Reif K, Safina BS, Salphati L, Staben S, Seward EM, Shuttleworth S, Sohal S, Sweeney ZK, Ultsch M, Waszkowycz B, Wei B.

Bioorg Med Chem Lett. 2012 Jul 1;22(13):4296-302. doi: 10.1016/j.bmcl.2012.05.027. Epub 2012 May 17.

PMID:
22672799
19.

Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.

Safina BS, Baker S, Baumgardner M, Blaney PM, Chan BK, Chen YH, Cartwright MW, Castanedo G, Chabot C, Cheguillaume AJ, Goldsmith P, Goldstein DM, Goyal B, Hancox T, Handa RK, Iyer PS, Kaur J, Kondru R, Kenny JR, Krintel SL, Li J, Lesnick J, Lucas MC, Lewis C, Mukadam S, Murray J, Nadin AJ, Nonomiya J, Padilla F, Palmer WS, Pang J, Pegg N, Price S, Reif K, Salphati L, Savy PA, Seward EM, Shuttleworth S, Sohal S, Sweeney ZK, Tay S, Tivitmahaisoon P, Waszkowycz B, Wei B, Yue Q, Zhang C, Sutherlin DP.

J Med Chem. 2012 Jun 28;55(12):5887-900. doi: 10.1021/jm3003747. Epub 2012 Jun 11.

PMID:
22626259
20.

Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling.

Chen H, Chan BK, Drummond J, Estrada AA, Gunzner-Toste J, Liu X, Liu Y, Moffat J, Shore D, Sweeney ZK, Tran T, Wang S, Zhao G, Zhu H, Burdick DJ.

J Med Chem. 2012 Jun 14;55(11):5536-45. doi: 10.1021/jm300452p. Epub 2012 Jun 1.

PMID:
22591441
21.

ACS chemical neuroscience spotlight on CEP-1347.

Sweeney ZK, Lewcock JW.

ACS Chem Neurosci. 2011 Jan 19;2(1):3-4. doi: 10.1021/cn1000793. Epub 2010 Sep 3. Review. No abstract available.

22.

Small-molecule inhibitors of store-operated calcium entry.

Sweeney ZK, Minatti A, Button DC, Patrick S.

ChemMedChem. 2009 May;4(5):706-18. doi: 10.1002/cmdc.200800452. Review.

PMID:
19330784
23.

Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.

Sweeney ZK, Harris SF, Arora SF, Javanbakht H, Li Y, Fretland J, Davidson JP, Billedeau JR, Gleason SK, Hirschfeld D, Kennedy-Smith JJ, Mirzadegan T, Roetz R, Smith M, Sperry S, Suh JM, Wu J, Tsing S, Villaseñor AG, Paul A, Su G, Heilek G, Hang JQ, Zhou AS, Jernelius JA, Zhang FJ, Klumpp K.

J Med Chem. 2008 Dec 11;51(23):7449-58. doi: 10.1021/jm800527x.

PMID:
19007201
24.

Diphenyl ether non-nucleoside reverse transcriptase inhibitors with excellent potency against resistant mutant viruses and promising pharmacokinetic properties.

Sweeney ZK, Kennedy-Smith JJ, Wu J, Arora N, Billedeau JR, Davidson JP, Fretland J, Hang JQ, Heilek GM, Harris SF, Hirschfeld D, Inbar P, Javanbakht H, Jernelius JA, Jin Q, Li Y, Liang W, Roetz R, Sarma K, Smith M, Stefanidis D, Su G, Suh JM, Villaseñor AG, Welch M, Zhang FJ, Klumpp K.

ChemMedChem. 2009 Jan;4(1):88-99. doi: 10.1002/cmdc.200800262.

PMID:
19006142
25.

Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.

Sweeney ZK, Dunn JP, Li Y, Heilek G, Dunten P, Elworthy TR, Han X, Harris SF, Hirschfeld DR, Hogg JH, Huber W, Kaiser AC, Kertesz DJ, Kim W, Mirzadegan T, Roepel MG, Saito YD, Silva TM, Swallow S, Tracy JL, Villasenor A, Vora H, Zhou AS, Klumpp K.

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4352-4. doi: 10.1016/j.bmcl.2008.06.072. Epub 2008 Jun 28.

PMID:
18632268
26.

Discovery of triazolinone non-nucleoside inhibitors of HIV reverse transcriptase.

Sweeney ZK, Acharya S, Briggs A, Dunn JP, Elworthy TR, Fretland J, Giannetti AM, Heilek G, Li Y, Kaiser AC, Martin M, Saito YD, Smith M, Suh JM, Swallow S, Wu J, Hang JQ, Zhou AS, Klumpp K.

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4348-51. doi: 10.1016/j.bmcl.2008.06.080. Epub 2008 Jun 28.

PMID:
18625554
27.
28.

Dihydrogen Activation by Titanium Sulfide Complexes.

Sweeney ZK, Polse JL, Bergman RG, Andersen RA.

Organometallics. 1999 Dec 20;18(26):5502-5510.

29.

Rearrangements and stereomutations of metallacycles derived from allenes and imidozirconium complexes.

Michael FE, Duncan AP, Sweeney ZK, Bergman RG.

J Am Chem Soc. 2005 Feb 16;127(6):1752-64.

30.

Mechanisms of allene stereoinversion by imidozirconium complexes.

Michael FE, Duncan AP, Sweeney ZK, Bergman RG.

J Am Chem Soc. 2003 Jun 18;125(24):7184-5.

31.

Highly enantioselective syntheses of homopropargylic alcohols and dihydrofurans catalyzed by a bis(oxazolinyl)pyridine-scandium triflate complex.

Evans DA, Sweeney ZK, Rovis T, Tedrow JS.

J Am Chem Soc. 2001 Dec 5;123(48):12095-6. No abstract available.

PMID:
11724622

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