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Items: 1 to 20 of 112

1.

Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome.

Blass BE, Iyer P, Abou-Gharbia M, Childers WE, Gordon JC, Ramanjulu M, Morton G, Arumugam P, Boruwa J, Ellingboe J, Mitra S, Nimmareddy RR, Paliwal S, Rajasekhar J, Shivakumar S, Srivastava P, Tangirala RS, Venkataramanaiah K, Yanamandra M.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5825-5829. doi: 10.1016/j.bmcl.2016.10.016. Epub 2016 Oct 10.

PMID:
27789139
2.

Identification and characterization of acidic mammalian chitinase inhibitors.

Cole DC, Olland AM, Jacob J, Brooks J, Bursavich MG, Czerwinski R, DeClercq C, Johnson M, Joseph-McCarthy D, Ellingboe JW, Lin L, Nowak P, Presman E, Strand J, Tam A, Williams CM, Yao S, Tsao DH, Fitz LJ.

J Med Chem. 2010 Aug 26;53(16):6122-8. doi: 10.1021/jm100533p.

PMID:
20666458
3.

Ion channel screening plates: design, construction, and maintenance.

Mayer SC, Butera JA, Diller DJ, Dunlop J, Ellingboe J, Fan KY, Kaftan E, Mekonnen B, Mobilio D, Paslay J, Tawa G, Vasilyev D, Bowlby MR.

Assay Drug Dev Technol. 2010 Aug;8(4):504-11. doi: 10.1089/adt.2009.0239.

PMID:
20470241
4.

Novel benzofuran derivatives with dual 5-HT1A receptor and serotonin transporter affinity.

Venkatesan AM, Dos Santos O, Ellingboe J, Evrard DA, Harrison BL, Smith DL, Scerni R, Hornby GA, Schechter LE, Andree TH.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):824-7. doi: 10.1016/j.bmcl.2009.12.093. Epub 2010 Jan 4.

PMID:
20064720
5.

Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists.

Cole DC, Gross JL, Comery TA, Aschmies S, Hirst WD, Kelley C, Kim JI, Kubek K, Ning X, Platt BJ, Robichaud AJ, Solvibile WR, Stock JR, Tawa G, Williams MJ, Ellingboe JW.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1237-40. doi: 10.1016/j.bmcl.2009.11.122. Epub 2009 Dec 4.

PMID:
20042333
6.

Identification of a new class of small molecule C5a receptor antagonists.

Chen JJ, Cole DC, Ciszewski G, Crouse K, Ellingboe JW, Nowak P, Tawa GJ, Berstein G, Li W.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):662-4. doi: 10.1016/j.bmcl.2009.11.058. Epub 2009 Dec 7.

PMID:
20004096
7.

Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors.

Nowak P, Cole DC, Aulabaugh A, Bard J, Chopra R, Cowling R, Fan KY, Hu B, Jacobsen S, Jani M, Jin G, Lo MC, Malamas MS, Manas ES, Narasimhan R, Reinhart P, Robichaud AJ, Stock JR, Subrath J, Svenson K, Turner J, Wagner E, Zhou P, Ellingboe JW.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):632-5. doi: 10.1016/j.bmcl.2009.11.052. Epub 2009 Nov 20.

PMID:
19959359
8.

Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.

Venkatesan AM, Dehnhardt CM, Chen Z, Santos ED, Dos Santos O, Bursavich M, Gilbert AM, Ellingboe JW, Ayral-Kaloustian S, Khafizova G, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Gibbons J, Abraham R, Mansour TS.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):653-6. doi: 10.1016/j.bmcl.2009.11.057. Epub 2009 Dec 1.

PMID:
19954970
9.

Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase.

Nowak P, Cole DC, Brooijmans N, Bursavich MG, Curran KJ, Ellingboe JW, Gibbons JJ, Hollander I, Hu Y, Kaplan J, Malwitz DJ, Toral-Barza L, Verheijen JC, Zask A, Zhang WG, Yu K.

J Med Chem. 2009 Nov 26;52(22):7081-9. doi: 10.1021/jm9012642.

PMID:
19848404
10.

Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.

Yu K, Toral-Barza L, Shi C, Zhang WG, Lucas J, Shor B, Kim J, Verheijen J, Curran K, Malwitz DJ, Cole DC, Ellingboe J, Ayral-Kaloustian S, Mansour TS, Gibbons JJ, Abraham RT, Nowak P, Zask A.

Cancer Res. 2009 Aug 1;69(15):6232-40. doi: 10.1158/0008-5472.CAN-09-0299. Epub 2009 Jul 7.

11.

Synthesis and activity of tryptophan sulfonamide derivatives as novel non-hydroxamate TNF-alpha converting enzyme (TACE) inhibitors.

Park K, Gopalsamy A, Aplasca A, Ellingboe JW, Xu W, Zhang Y, Levin JI.

Bioorg Med Chem. 2009 Jun 1;17(11):3857-65. doi: 10.1016/j.bmc.2009.04.033. Epub 2009 Apr 22.

PMID:
19410464
12.

(S)-N-(5-Chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol a Notch-1-sparing gamma-secretase inhibitor.

Cole DC, Stock JR, Kreft AF, Antane M, Aschmies SH, Atchison KP, Casebier DS, Comery TA, Diamantidis G, Ellingboe JW, Harrison BL, Hu Y, Jin M, Kubrak DM, Lu P, Mann CW, Martone RL, Moore WJ, Oganesian A, Riddell DR, Sonnenberg-Reines J, Sun SC, Wagner E, Wang Z, Woller KR, Xu Z, Zhou H, Jacobsen JS.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):926-9. doi: 10.1016/j.bmcl.2008.11.116. Epub 2008 Dec 6.

PMID:
19097890
13.

Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.

Mayer SC, Kreft AF, Harrison B, Abou-Gharbia M, Antane M, Aschmies S, Atchison K, Chlenov M, Cole DC, Comery T, Diamantidis G, Ellingboe J, Fan K, Galante R, Gonzales C, Ho DM, Hoke ME, Hu Y, Huryn D, Jain U, Jin M, Kremer K, Kubrak D, Lin M, Lu P, Magolda R, Martone R, Moore W, Oganesian A, Pangalos MN, Porte A, Reinhart P, Resnick L, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Wang T, Woller K, Xu Z, Zaleska MM, Zeldis J, Zhang M, Zhou H, Jacobsen JS.

J Med Chem. 2008 Dec 11;51(23):7348-51. doi: 10.1021/jm801252w.

PMID:
19012391
14.

Identification, characterization and initial hit-to-lead optimization of a series of 4-arylamino-3-pyridinecarbonitrile as protein kinase C theta (PKCtheta) inhibitors.

Cole DC, Asselin M, Brennan A, Czerwinski R, Ellingboe JW, Fitz L, Greco R, Huang X, Joseph-McCarthy D, Kelly MF, Kirisits M, Lee J, Li Y, Morgan P, Stock JR, Tsao DH, Wissner A, Yang X, Chaudhary D.

J Med Chem. 2008 Oct 9;51(19):5958-63. doi: 10.1021/jm800214a. Epub 2008 Sep 11.

PMID:
18783200
15.

Discovery of a novel series of Notch-sparing gamma-secretase inhibitors.

Kreft A, Harrison B, Aschmies S, Atchison K, Casebier D, Cole DC, Diamantidis G, Ellingboe J, Hauze D, Hu Y, Huryn D, Jin M, Kubrak D, Lu P, Lundquist J, Mann C, Martone R, Moore W, Oganesian A, Porte A, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Woller K, Xu Z, Zhou H, Steven Jacobsen J.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4232-6. doi: 10.1016/j.bmcl.2008.05.064. Epub 2008 May 20.

PMID:
18556202
16.

Discovery of benzisoxazoles as potent inhibitors of chaperone heat shock protein 90.

Gopalsamy A, Shi M, Golas J, Vogan E, Jacob J, Johnson M, Lee F, Nilakantan R, Petersen R, Svenson K, Chopra R, Tam MS, Wen Y, Ellingboe J, Arndt K, Boschelli F.

J Med Chem. 2008 Feb 14;51(3):373-5. doi: 10.1021/jm701385c. Epub 2008 Jan 16.

PMID:
18197612
17.

Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.

Cole DC, Stock JR, Chopra R, Cowling R, Ellingboe JW, Fan KY, Harrison BL, Hu Y, Jacobsen S, Jennings LD, Jin G, Lohse PA, Malamas MS, Manas ES, Moore WJ, O'Donnell MM, Olland AM, Robichaud AJ, Svenson K, Wu J, Wagner E, Bard J.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):1063-6. Epub 2007 Dec 10.

PMID:
18162398
18.

Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.

Jennings LD, Cole DC, Stock JR, Sukhdeo MN, Ellingboe JW, Cowling R, Jin G, Manas ES, Fan KY, Malamas MS, Harrison BL, Jacobsen S, Chopra R, Lohse PA, Moore WJ, O'Donnell MM, Hu Y, Robichaud AJ, Turner MJ, Wagner E, Bard J.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):767-71. Epub 2007 Nov 17.

PMID:
18068983
19.

Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.

Cole DC, Stock JR, Lennox WJ, Bernotas RC, Ellingboe JW, Boikess S, Coupet J, Smith DL, Leung L, Zhang GM, Feng X, Kelly MF, Galante R, Huang P, Dawson LA, Marquis K, Rosenzweig-Lipson S, Beyer CE, Schechter LE.

J Med Chem. 2007 Nov 15;50(23):5535-8. Epub 2007 Oct 19.

PMID:
17948978
20.

Acylguanidines as small-molecule beta-secretase inhibitors.

Cole DC, Manas ES, Stock JR, Condon JS, Jennings LD, Aulabaugh A, Chopra R, Cowling R, Ellingboe JW, Fan KY, Harrison BL, Hu Y, Jacobsen S, Jin G, Lin L, Lovering FE, Malamas MS, Stahl ML, Strand J, Sukhdeo MN, Svenson K, Turner MJ, Wagner E, Wu J, Zhou P, Bard J.

J Med Chem. 2006 Oct 19;49(21):6158-61.

PMID:
17034121

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