Format
Sort by
Items per page

Send to

Choose Destination

Links from PubMed

Items: 1 to 20 of 79

1.

Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).

Seal J, Lamotte Y, Donche F, Bouillot A, Mirguet O, Gellibert F, Nicodeme E, Krysa G, Kirilovsky J, Beinke S, McCleary S, Rioja I, Bamborough P, Chung CW, Gordon L, Lewis T, Walker AL, Cutler L, Lugo D, Wilson DM, Witherington J, Lee K, Prinjha RK.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72. doi: 10.1016/j.bmcl.2012.02.041. Epub 2012 Feb 24.

PMID:
22437115
2.

From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.

Mirguet O, Lamotte Y, Donche F, Toum J, Gellibert F, Bouillot A, Gosmini R, Nguyen VL, Delannée D, Seal J, Blandel F, Boullay AB, Boursier E, Martin S, Brusq JM, Krysa G, Riou A, Tellier R, Costaz A, Huet P, Dudit Y, Trottet L, Kirilovsky J, Nicodeme E.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2963-7. doi: 10.1016/j.bmcl.2012.01.125. Epub 2012 Feb 8.

PMID:
22386529
3.

Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: chemistry, biological activities, and molecular modeling.

Tong Y, Stewart KD, Thomas S, Przytulinska M, Johnson EF, Klinghofer V, Leverson J, McCall O, Soni NB, Luo Y, Lin NH, Sowin TJ, Giranda VL, Penning TD.

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5206-8. doi: 10.1016/j.bmcl.2008.08.079. Epub 2008 Aug 28.

PMID:
18790640
4.

Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene.

Bass JY, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, McFadyen RB, Miller AB, Mills WY, Navas F 3rd, Parks DJ, Smalley TL Jr, Spearing PK, Todd D, Williams SP, Wisely GB.

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1206-13. doi: 10.1016/j.bmcl.2010.12.089. Epub 2010 Dec 23.

PMID:
21256005
5.

An efficient one-pot, three-component synthesis of indeno[1,2-b]quinoline-9,11(6H,10H)-dione, acridine-1,8(2H,5H)-dione and quinoline-3-carbonitrile derivatives from enaminones.

Tu SJ, Jiang B, Jia RH, Zhang JY, Zhang Y, Yao CS, Shi F.

Org Biomol Chem. 2006 Oct 7;4(19):3664-8. Epub 2006 Aug 17.

PMID:
16990942
6.

Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.

Andrés JI, Alcázar J, Alonso JM, Alvarez RM, Bakker MH, Biesmans I, Cid JM, De Lucas AI, Fernández J, Font LM, Hens KA, Iturrino L, Lenaerts I, Martínez S, Megens AA, Pastor J, Vermote PC, Steckler T.

J Med Chem. 2005 Mar 24;48(6):2054-71.

PMID:
15771448
7.

Synthesis, high-resolution NMR spectroscopic analysis, and single-crystal X-ray diffraction of isoxazoline tetracycles.

Fascio ML, Alvarez-Larena A, D'Accorso NB.

Carbohydr Res. 2002 Nov 29;337(24):2419-25.

PMID:
12493226
8.

Fragment-based discovery of bromodomain inhibitors part 2: optimization of phenylisoxazole sulfonamides.

Bamborough P, Diallo H, Goodacre JD, Gordon L, Lewis A, Seal JT, Wilson DM, Woodrow MD, Chung CW.

J Med Chem. 2012 Jan 26;55(2):587-96. doi: 10.1021/jm201283q. Epub 2012 Jan 11.

PMID:
22136469
9.

Identification of an N-oxide pyridine GW4064 analog as a potent FXR agonist.

Feng S, Yang M, Zhang Z, Wang Z, Hong D, Richter H, Benson GM, Bleicher K, Grether U, Martin RE, Plancher JM, Kuhn B, Rudolph MG, Chen L.

Bioorg Med Chem Lett. 2009 May 1;19(9):2595-8. doi: 10.1016/j.bmcl.2009.03.008. Epub 2009 Mar 9.

PMID:
19328688
10.

The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.

Gosmini R, Nguyen VL, Toum J, Simon C, Brusq JM, Krysa G, Mirguet O, Riou-Eymard AM, Boursier EV, Trottet L, Bamborough P, Clark H, Chung CW, Cutler L, Demont EH, Kaur R, Lewis AJ, Schilling MB, Soden PE, Taylor S, Walker AL, Walker MD, Prinjha RK, Nicodème E.

J Med Chem. 2014 Oct 9;57(19):8111-31. doi: 10.1021/jm5010539. Epub 2014 Sep 24.

PMID:
25249180
11.

Structure-activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating Mycobacterium tuberculosis.

Lilienkampf A, Mao J, Wan B, Wang Y, Franzblau SG, Kozikowski AP.

J Med Chem. 2009 Apr 9;52(7):2109-18. doi: 10.1021/jm900003c.

PMID:
19271749
12.

Isoxazole to oxazole: a mild and unexpected transformation.

Jones RC, Chatterley A, Marty R, Owton WM, Elsegood MR.

Chem Commun (Camb). 2015 Jan 21;51(6):1112-5. doi: 10.1039/c4cc07999j.

PMID:
25461278
13.

Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors.

Zhao H, Liu G, Xin Z, Serby MD, Pei Z, Szczepankiewicz BG, Hajduk PJ, Abad-Zapatero C, Hutchins CW, Lubben TH, Ballaron SJ, Haasch DL, Kaszubska W, Rondinone CM, Trevillyan JM, Jirousek MR.

Bioorg Med Chem Lett. 2004 Nov 15;14(22):5543-6.

PMID:
15482920
14.

New nonpeptide angiotensin II receptor antagonists. 2. Synthesis, biological properties, and structure-activity relationships of 2-alkyl-4-(biphenylylmethoxy)quinoline derivatives.

Bradbury RH, Allott CP, Dennis M, Fisher E, Major JS, Masek BB, Oldham AA, Pearce RJ, Rankine N, Revill JM, et al.

J Med Chem. 1992 Oct 30;35(22):4027-38.

PMID:
1433210
15.

An efficient one-pot synthesis and photoinduced DNA cleavage studies of 2-chloro-3-(5-aryl-4,5-dihydroisoxazol-3-yl)quinolines.

Bindu PJ, Mahadevan KM, Ravikumar Naik TR.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6095-8. doi: 10.1016/j.bmcl.2012.08.034. Epub 2012 Aug 17.

PMID:
22959207
16.

The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS).

Cheshire DR, Åberg A, Andersson GM, Andrews G, Beaton HG, Birkinshaw TN, Boughton-Smith N, Connolly S, Cook TR, Cooper A, Cooper SL, Cox D, Dixon J, Gensmantel N, Hamley PJ, Harrison R, Hartopp P, Käck H, Leeson PD, Luker T, Mete A, Millichip I, Nicholls DJ, Pimm AD, St-Gallay SA, Wallace AV.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2468-71. doi: 10.1016/j.bmcl.2011.02.061. Epub 2011 Feb 18.

PMID:
21398123
17.

Synthesis, in vitro antitumor evaluation and DNA-binding study of novel tetrahydroquinolines and some derived tricyclic and tetracyclic ring systems.

Faidallah HM, Rostom SA.

Eur J Med Chem. 2013 May;63:133-43. doi: 10.1016/j.ejmech.2013.02.006. Epub 2013 Feb 16.

PMID:
23474899
18.

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762.

Chaidos A, Caputo V, Gouvedenou K, Liu B, Marigo I, Chaudhry MS, Rotolo A, Tough DF, Smithers NN, Bassil AK, Chapman TD, Harker NR, Barbash O, Tummino P, Al-Mahdi N, Haynes AC, Cutler L, Le B, Rahemtulla A, Roberts I, Kleijnen M, Witherington JJ, Parr NJ, Prinjha RK, Karadimitris A.

Blood. 2014 Jan 30;123(5):697-705. doi: 10.1182/blood-2013-01-478420. Epub 2013 Dec 13.

19.

Discovery of 4-Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38.

Becherer JD, Boros EE, Carpenter TY, Cowan DJ, Deaton DN, Haffner CD, Jeune MR, Kaldor IW, Poole JC, Preugschat F, Rheault TR, Schulte CA, Shearer BG, Shearer TW, Shewchuk LM, Smalley TL Jr, Stewart EL, Stuart JD, Ulrich JC.

J Med Chem. 2015 Sep 10;58(17):7021-56. doi: 10.1021/acs.jmedchem.5b00992. Epub 2015 Aug 24.

PMID:
26267483
20.

A fluorinated analog of ISO-1 blocks the recognition and biological function of MIF and is orally efficacious in a murine model of colitis.

Dagia NM, Kamath DV, Bhatt P, Gupte RD, Dadarkar SS, Fonseca L, Agarwal G, Chetrapal-Kunwar A, Balachandran S, Srinivasan S, Bose J, Pari K, B-Rao C, Parkale SS, Gadekar PK, Rodge AH, Mandrekar N, Vishwakarma RA, Sharma S.

Eur J Pharmacol. 2009 Apr 1;607(1-3):201-12. doi: 10.1016/j.ejphar.2009.02.031. Epub 2009 Feb 21.

PMID:
19239912

Supplemental Content

Support Center