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Items: 1 to 20 of 112

1.

Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity.

Diallo H, Angell DC, Barnett HA, Biggadike K, Coe DM, Cooper TW, Craven A, Gray JR, House D, Jack TI, Keeling SP, Macdonald SJ, McLay IM, Oliver S, Taylor SJ, Uings IJ, Wellaway N.

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1126-33. doi: 10.1016/j.bmcl.2010.12.121. Epub 2010 Dec 31.

PMID:
21257309
2.

Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists.

Gilmore JL, Sheppeck JE 2nd, Wang J, Dhar TG, Cavallaro C, Doweyko AM, Mckay L, Cunningham MD, Habte SF, Nadler SG, Dodd JH, Somerville JE, Barrish JC.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5448-51. doi: 10.1016/j.bmcl.2013.06.085. Epub 2013 Jul 4.

PMID:
23916594
3.

Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.

Biggadike K, Caivano M, Clackers M, Coe DM, Hardy GW, Humphreys D, Jones HT, House D, Miles-Williams A, Skone PA, Uings I, Weller V, McLay IM, Macdonald SJ.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4846-50. doi: 10.1016/j.bmcl.2009.06.020. Epub 2009 Jun 13.

PMID:
19592247
4.

Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.

Clackers M, Coe DM, Demaine DA, Hardy GW, Humphreys D, Inglis GG, Johnston MJ, Jones HT, House D, Loiseau R, Minick DJ, Skone PA, Uings I, McLay IM, Macdonald SJ.

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4737-45. Epub 2007 Jun 26.

PMID:
17616395
5.

5-Functionalized indazoles as glucocorticoid receptor agonists.

Bai M, Carr G, Deorazio RJ, Friedrich TD, Dobritsa S, Fitzpatrick K, Guzzo PR, Kitchen DB, Lynch MA, Peace D, Sajad M, Usyatinsky A, Wolf MA.

Bioorg Med Chem Lett. 2010 May 15;20(10):3017-20. doi: 10.1016/j.bmcl.2010.04.012. Epub 2010 Apr 11.

PMID:
20427184
6.

Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists.

Sheppeck JE 2nd, Gilmore JL, Xiao HY, Dhar TG, Nirschl D, Doweyko AM, Sack JS, Corbett MJ, Malley MF, Gougoutas JZ, Mckay L, Cunningham MD, Habte SF, Dodd JH, Nadler SG, Somerville JE, Barrish JC.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5442-7. doi: 10.1016/j.bmcl.2013.06.089. Epub 2013 Jul 9.

PMID:
23953070
7.

Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.

Yates CM, Brown PJ, Stewart EL, Patten C, Austin RJ, Holt JA, Maglich JM, Angell DC, Sasse RZ, Taylor SJ, Uings IJ, Trump RP.

J Med Chem. 2010 Jun 10;53(11):4531-44. doi: 10.1021/jm100447c.

PMID:
20469868
8.

Lead optimisation of the N1 substituent of a novel series of indazole arylsulfonamides as CCR4 antagonists and identification of a candidate for clinical investigation.

Procopiou PA, Ford AJ, Graves RH, Hall DA, Hodgson ST, Lacroix YM, Needham D, Slack RJ.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2730-3. doi: 10.1016/j.bmcl.2012.02.104. Epub 2012 Mar 7.

PMID:
22437117
9.

Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity.

Ali A, Thompson CF, Balkovec JM, Graham DW, Hammond ML, Quraishi N, Tata JR, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Thompson CM, Zaller DM, Forrest MJ, Carballo-Jane E, Luell S.

J Med Chem. 2004 May 6;47(10):2441-52.

PMID:
15115388
10.

Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist.

Brown AR, Bosies M, Cameron H, Clark J, Cowley A, Craighead M, Elmore MA, Firth A, Goodwin R, Goutcher S, Grant E, Grassie M, Grove SJ, Hamilton NM, Hampson H, Hillier A, Ho KK, Kiczun M, Kingsbury C, Kultgen SG, Littlewood PT, Lusher SJ, Macdonald S, McIntosh L, McIntyre T, Mistry A, Morphy JR, Nimz O, Ohlmeyer M, Pick J, Rankovic Z, Sherborne B, Smith A, Speake M, Spinks G, Thomson F, Watson L, Weston M.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):137-40. doi: 10.1016/j.bmcl.2010.11.054. Epub 2010 Nov 16.

PMID:
21129964
11.

Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity.

Roach SL, Higuchi RI, Hudson AR, Adams ME, Syka PM, Mais DE, Miner JN, Marschke KB, Zhi L.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):168-71. doi: 10.1016/j.bmcl.2010.11.047. Epub 2010 Nov 11.

PMID:
21115247
12.

The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation.

Edman K, Ahlgren R, Bengtsson M, Bladh H, Bäckström S, Dahmén J, Henriksson K, Hillertz P, Hulikal V, Jerre A, Kinchin L, Kåse C, Lepistö M, Mile I, Nilsson S, Smailagic A, Taylor J, Tjörnebo A, Wissler L, Hansson T.

Bioorg Med Chem Lett. 2014 Jun 1;24(11):2571-7. doi: 10.1016/j.bmcl.2014.03.070. Epub 2014 Apr 2.

PMID:
24755427
13.

Structure-based design, synthesis, and antimicrobial activity of indazole-derived SAH/MTA nucleosidase inhibitors.

Li X, Chu S, Feher VA, Khalili M, Nie Z, Margosiak S, Nikulin V, Levin J, Sprankle KG, Tedder ME, Almassy R, Appelt K, Yager KM.

J Med Chem. 2003 Dec 18;46(26):5663-73.

PMID:
14667220
14.

Substituted phenyl as a steroid A-ring mimetic: providing agonist activity to a class of arylsulfonamide nonsteroidal glucocorticoid ligands.

DiSalvo D, Kuzmich D, Bentzien J, Regan J, Kukulka A, Fadra-Khan T, Nelson R, Harcken C, Thomson D, Nabozny G.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6645-9. doi: 10.1016/j.bmcl.2013.10.047. Epub 2013 Oct 31.

PMID:
24239189
15.

Synthesis and biological evaluation of N-(7-indazolyl)benzenesulfonamide derivatives as potent cell cycle inhibitors.

Bouissane L, El Kazzouli S, Léonce S, Pfeiffer B, Rakib EM, Khouili M, Guillaumet G.

Bioorg Med Chem. 2006 Feb 15;14(4):1078-88. Epub 2005 Nov 7.

PMID:
16274996
16.

Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators.

Hemmerling M, Edman K, Lepistö M, Eriksson A, Ivanova S, Dahmén J, Rehwinkel H, Berger M, Hendrickx R, Dearman M, Jensen TJ, Wissler L, Hansson T.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5741-5748. doi: 10.1016/j.bmcl.2016.10.052. Epub 2016 Oct 19.

PMID:
27810243
17.

Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists.

Procopiou PA, Barrett JW, Barton NP, Begg M, Clapham D, Copley RC, Ford AJ, Graves RH, Hall DA, Hancock AP, Hill AP, Hobbs H, Hodgson ST, Jumeaux C, Lacroix YM, Miah AH, Morriss KM, Needham D, Sheriff EB, Slack RJ, Smith CE, Sollis SL, Staton H.

J Med Chem. 2013 Mar 14;56(5):1946-60. doi: 10.1021/jm301572h. Epub 2013 Feb 27.

PMID:
23409871
18.

Alpha-methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands.

Marshall DR, Rodriguez G, Thomson DS, Nelson R, Capolina A.

Bioorg Med Chem Lett. 2007 Jan 15;17(2):315-9. Epub 2006 Oct 25.

PMID:
17118655
19.

1,3-diaminopropan-2-ol sulfonamides as potent and selective inhibitors of the glycine transporter type 1.

Rahman SS, Coulton S, Herdon HJ, Joiner GF, Jin J, Porter RA.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1741-5. Epub 2006 Dec 22.

PMID:
17234406
20.

Discovery and optimization of novel, non-steroidal glucocorticoid receptor modulators.

Ray NC, Clark RD, Clark DE, Williams K, Hickin HG, Crackett PH, Dyke HJ, Lockey PM, Wong M, Devos R, White A, Belanoff JK.

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4901-5. Epub 2007 Jun 13.

PMID:
17587578

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