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Items: 1 to 20 of 114

1.

Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists.

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

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1697-700. doi: 10.1016/j.bmcl.2011.01.093.

PMID:
21316964
2.

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.

PMID:
21115247
3.

Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists.

Takahashi H, Bekkali Y, Capolino AJ, Gilmore T, Goldrick SE, Kaplita PV, Liu L, Nelson RM, Terenzio D, Wang J, Zuvela-Jelaska L, Proudfoot J, Nabozny G, Thomson D.

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5091-5.

PMID:
17681466
4.

Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation.

Hudson AR, Higuchi RI, Roach SL, Valdez LJ, Adams ME, Vassar A, Rungta D, Syka PM, Mais DE, Marschke KB, Zhi L.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1654-7. doi: 10.1016/j.bmcl.2011.01.104.

PMID:
21324689
5.

Discovery of quinolines as selective glucocorticoid receptor agonists.

Jaroch S, Berger M, Huwe C, Krolikiewicz K, Rehwinkel H, Schäcke H, Schmees N, Skuballa W.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5835-8. doi: 10.1016/j.bmcl.2010.07.125.

PMID:
20727743
6.

Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.

Roach SL, Higuchi RI, Adams ME, Liu Y, Karanewsky DS, Marschke KB, Mais DE, Miner JN, Zhi L.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3504-8. doi: 10.1016/j.bmcl.2008.05.029.

PMID:
18513967
7.

Steroidal C-21 heteroaryl thioethers (Part 2): discovery of orally bioavailable selective glucocorticoid receptor modulators (dissociated steroids).

Biju P, McCormick K, Aslanian R, Berlin M, Solomon D, Wang H, Lee YJ, Bitar R, Prelusky D, McLeod R, Jia Y, Fernandez X, Eckel S, House A, Lieber G, Jimenez J, Kelly G, Chapman R, Phillips J, Anthes J.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1086-90. doi: 10.1016/j.bmcl.2011.11.120.

PMID:
22197391
8.

Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation.

Roach SL, Higuchi RI, Hudson AR, Vassar A, Grant VH, Lamer R, Hooper C, Rungta D, Syka PM, Mais DE, Marschke KB, Zhi L.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1658-62. doi: 10.1016/j.bmcl.2011.01.106.

PMID:
21349714
9.

Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.

Kym PR, Kort ME, Coghlan MJ, Moore JL, Tang R, Ratajczyk JD, Larson DP, Elmore SW, Pratt JK, Stashko MA, Falls HD, Lin CW, Nakane M, Miller L, Tyree CM, Miner JN, Jacobson PB, Wilcox DM, Nguyen P, Lane BC.

J Med Chem. 2003 Mar 13;46(6):1016-30.

PMID:
12620078
10.

Quinolines as a novel structural class of potent and selective PDE4 inhibitors: optimisation for oral administration.

Lunniss CJ, Cooper AW, Eldred CD, Kranz M, Lindvall M, Lucas FS, Neu M, Preston AG, Ranshaw LE, Redgrave AJ, Ed Robinson J, Shipley TJ, Solanke YE, Somers DO, Wiseman JO.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1380-5. doi: 10.1016/j.bmcl.2009.01.045.

PMID:
19195882
11.

5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.

Zhi L, Tegley CM, Kallel EA, Marschke KB, Mais DE, Gottardis MM, Jones TK.

J Med Chem. 1998 Jan 29;41(3):291-302.

PMID:
9464360
12.

Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.

Hudson AR, Roach SL, Higuchi RI, Phillips DP, Bissonnette RP, Lamph WW, Yen J, Li Y, Adams ME, Valdez LJ, Vassar A, Cuervo C, Kallel EA, Gharbaoui CJ, Mais DE, Miner JN, Marschke KB, Rungta D, Negro-Vilar A, Zhi L.

J Med Chem. 2007 Sep 20;50(19):4699-709.

PMID:
17705362
13.

Combining 3D-QSAR, docking, molecular dynamics and MM/PBSA methods to predict binding modes for nonsteroidal selective modulator to glucocorticoid receptor.

Xu Y, Zhang T, Chen M.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):393-6. doi: 10.1016/j.bmcl.2008.11.069.

PMID:
19081253
14.

Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.

Elmore SW, Coghlan MJ, Anderson DD, Pratt JK, Green BE, Wang AX, Stashko MA, Lin CW, Tyree CM, Miner JN, Jacobson PB, Wilcox DM, Lane BC.

J Med Chem. 2001 Dec 6;44(25):4481-91.

PMID:
11728194
15.

Tetrahydroquinoline derivatives as CRTH2 antagonists.

Liu J, Wang Y, Sun Y, Marshall D, Miao S, Tonn G, Anders P, Tocker J, Tang HL, Medina J.

Bioorg Med Chem Lett. 2009 Dec 15;19(24):6840-4. doi: 10.1016/j.bmcl.2009.10.094.

PMID:
19896843
16.

Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.

Barker M, Clackers M, Copley R, Demaine DA, Humphreys D, Inglis GG, Johnston MJ, Jones HT, Haase MV, House D, Loiseau R, Nisbet L, Pacquet F, Skone PA, Shanahan SE, Tape D, Vinader VM, Washington M, Uings I, Upton R, McLay IM, Macdonald SJ.

J Med Chem. 2006 Jul 13;49(14):4216-31.

PMID:
16821781
17.

Discovery of liver selective non-steroidal glucocorticoid receptor antagonist as novel antidiabetic agents.

Shah K, Patel D, Jadav P, Sheikh M, Sairam KV, Joharapurkar A, Jain MR, Bahekar R.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5857-62. doi: 10.1016/j.bmcl.2012.07.078.

PMID:
22917520
18.

Design, synthesis, and structure-activity relationships of a series of 2-Ar-8-methyl-5-alkylaminoquinolines as novel CRF₁ receptor antagonists.

Takeda K, Terauchi T, Hashizume M, Shin K, Ino M, Shibata H, Yonaga M.

Bioorg Med Chem Lett. 2012 Sep 1;22(17):5372-8. doi: 10.1016/j.bmcl.2012.07.047.

PMID:
22871582
19.

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
20.

Tetrahydroquinoline derivatives as opioid receptor antagonists.

Zhang C, Westaway SM, Speake JD, Bishop MJ, Goetz AS, Carballo LH, Hu M, Epperly AH.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):670-6. doi: 10.1016/j.bmcl.2010.12.010.

PMID:
21193310
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