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Items: 1 to 20 of 105

1.

Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.

Xue CB, Chen L, Cao G, Zhang K, Wang A, Meloni D, Glenn J, Anand R, Xia M, Kong L, Huang T, Feng H, Zheng C, Li M, Galya L, Zhou J, Shin N, Baribaud F, Solomon K, Scherle P, Zhao B, Diamond S, Emm T, Keller D, Contel N, Yeleswaram S, Vaddi K, Hollis G, Newton R, Friedman S, Metcalf B.

ACS Med Chem Lett. 2010 Aug 25;1(9):483-7. doi: 10.1021/ml1001536. eCollection 2010 Dec 9.

2.

Identification and characterization of INCB9471, an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5 with potent inhibitory activity against monocyte migration and HIV-1 infection.

Shin N, Solomon K, Zhou N, Wang KH, Garlapati V, Thomas B, Li Y, Covington M, Baribaud F, Erickson-Viitanen S, Czerniak P, Contel N, Liu P, Burn T, Hollis G, Yeleswaram S, Vaddi K, Xue CB, Metcalf B, Friedman S, Scherle P, Newton R.

J Pharmacol Exp Ther. 2011 Jul;338(1):228-39. doi: 10.1124/jpet.111.179531. Epub 2011 Apr 1.

3.

SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo.

Strizki JM, Xu S, Wagner NE, Wojcik L, Liu J, Hou Y, Endres M, Palani A, Shapiro S, Clader JW, Greenlee WJ, Tagat JR, McCombie S, Cox K, Fawzi AB, Chou CC, Pugliese-Sivo C, Davies L, Moreno ME, Ho DD, Trkola A, Stoddart CA, Moore JP, Reyes GR, Baroudy BM.

Proc Natl Acad Sci U S A. 2001 Oct 23;98(22):12718-23. Epub 2001 Oct 16.

4.

Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity.

Dorr P, Westby M, Dobbs S, Griffin P, Irvine B, Macartney M, Mori J, Rickett G, Smith-Burchnell C, Napier C, Webster R, Armour D, Price D, Stammen B, Wood A, Perros M.

Antimicrob Agents Chemother. 2005 Nov;49(11):4721-32.

5.

Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity.

Palani A, Shapiro S, Josien H, Bara T, Clader JW, Greenlee WJ, Cox K, Strizki JM, Baroudy BM.

J Med Chem. 2002 Jul 4;45(14):3143-60.

PMID:
12086500
6.
9.

Recent advances of CCR5 antagonists.

Baba M.

Curr Opin HIV AIDS. 2006 Sep;1(5):367-72. doi: 10.1097/01.COH.0000239848.13205.2a.

PMID:
19372835
10.

Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety.

Seto M, Aikawa K, Miyamoto N, Aramaki Y, Kanzaki N, Takashima K, Kuze Y, Iizawa Y, Baba M, Shiraishi M.

J Med Chem. 2006 Mar 23;49(6):2037-48.

PMID:
16539392
11.

Discovery of a potent, selective and orally bioavailable 3,9-diazaspiro[5.5]undeca-2-one CCR5 antagonist.

Yang H, Lin XF, Padilla F, Gabriel SD, Heilek G, Ji C, Sankuratri S, deRosier A, Berry P, Rotstein DM.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):209-13. doi: 10.1016/j.bmcl.2008.10.115. Epub 2008 Oct 31.

PMID:
19014885
12.

Highly potent inhibition of human immunodeficiency virus type 1 replication by TAK-220, an orally bioavailable small-molecule CCR5 antagonist.

Takashima K, Miyake H, Kanzaki N, Tagawa Y, Wang X, Sugihara Y, Iizawa Y, Baba M.

Antimicrob Agents Chemother. 2005 Aug;49(8):3474-82.

13.

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.

Shen DM, Shu M, Willoughby CA, Shah S, Lynch CL, Hale JJ, Mills SG, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):941-5.

PMID:
15012998
14.

HIV co-receptors as targets for antiviral therapy.

Schols D.

Curr Top Med Chem. 2004;4(9):883-93. Review.

PMID:
15134547
15.

Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1.

Strizki JM, Tremblay C, Xu S, Wojcik L, Wagner N, Gonsiorek W, Hipkin RW, Chou CC, Pugliese-Sivo C, Xiao Y, Tagat JR, Cox K, Priestley T, Sorota S, Huang W, Hirsch M, Reyes GR, Baroudy BM.

Antimicrob Agents Chemother. 2005 Dec;49(12):4911-9.

16.

Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.

Xue CB, Wang A, Han Q, Zhang Y, Cao G, Feng H, Huang T, Zheng C, Xia M, Zhang K, Kong L, Glenn J, Anand R, Meloni D, Robinson DJ, Shao L, Storace L, Li M, Hughes RO, Devraj R, Morton PA, Rogier DJ, Covington M, Scherle P, Diamond S, Emm T, Yeleswaram S, Contel N, Vaddi K, Newton R, Hollis G, Metcalf B.

ACS Med Chem Lett. 2011 Oct 5;2(12):913-8. doi: 10.1021/ml200199c. eCollection 2011 Dec 8.

17.

Cenicriviroc, an orally active CCR5 antagonist for the potential treatment of HIV infection.

Klibanov OM, Williams SH, Iler CA.

Curr Opin Investig Drugs. 2010 Aug;11(8):940-50.

PMID:
20721836
18.

The lupane-type triterpene 30-oxo-calenduladiol is a CCR5 antagonist with anti-HIV-1 and anti-chemotactic activities.

Barroso-González J, El Jaber-Vazdekis N, García-Expósito L, Machado JD, Zárate R, Ravelo AG, Estévez-Braun A, Valenzuela-Fernández A.

J Biol Chem. 2009 Jun 12;284(24):16609-20. doi: 10.1074/jbc.M109.005835. Epub 2009 Apr 22.

19.

P2X1 Receptor Antagonists Inhibit HIV-1 Fusion by Blocking Virus-Coreceptor Interactions.

Giroud C, Marin M, Hammonds J, Spearman P, Melikyan GB.

J Virol. 2015 Sep;89(18):9368-82. doi: 10.1128/JVI.01178-15. Epub 2015 Jul 1.

20.

Synthesis and biological evaluation of 1,3,3,4-tetrasubstituted pyrrolidine CCR5 receptor antagonists. Discovery of a potent and orally bioavailable anti-HIV agent.

Ma D, Yu S, Li B, Chen L, Chen R, Yu K, Zhang L, Chen Z, Zhong D, Gong Z, Wang R, Jiang H, Pei G.

ChemMedChem. 2007 Feb;2(2):187-93.

PMID:
17163560

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