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Items: 24

1.

Highlights of the Structure-Activity Relationships of Benzimidazole Linked Pyrrolidines Leading to the Discovery of the Hepatitis C Virus NS5A Inhibitor Pibrentasvir (ABT-530).

Wagner R, Randolph JT, Patel SV, Nelson L, Matulenko MA, Keddy R, Pratt JK, Liu D, Krueger AC, Donner PL, Hutchinson DK, Flentge C, Betebenner D, Rockway T, Maring CJ, Ng TI, Krishnan P, Pilot-Matias T, Collins C, Panchal N, Reisch T, Dekhtyar T, Mondal R, Stolarik DF, Gao Y, Gao W, Beno DA, Kati WM.

J Med Chem. 2018 May 10;61(9):4052-4066. doi: 10.1021/acs.jmedchem.8b00082. Epub 2018 Apr 23.

PMID:
29653491
2.

Synthesis and Biological Characterization of Aryl Uracil Inhibitors of Hepatitis C Virus NS5B Polymerase: Discovery of ABT-072, a trans-Stilbene Analog with Good Oral Bioavailability.

Randolph JT, Krueger AC, Donner PL, Pratt JK, Liu D, Motter CE, Rockway TW, Tufano MD, Wagner R, Lim HB, Beyer JM, Mondal R, Panchal NS, Colletti L, Liu Y, Koev G, Kati WM, Hernandez LE, Beno DWA, Longenecker KL, Stewart KD, Dumas EO, Molla A, Maring CJ.

J Med Chem. 2018 Feb 8;61(3):1153-1163. doi: 10.1021/acs.jmedchem.7b01630. Epub 2018 Jan 25.

PMID:
29342358
3.

In Vitro Antiviral Activity and Resistance Profile of the Next-Generation Hepatitis C Virus NS5A Inhibitor Pibrentasvir.

Ng TI, Krishnan P, Pilot-Matias T, Kati W, Schnell G, Beyer J, Reisch T, Lu L, Dekhtyar T, Irvin M, Tripathi R, Maring C, Randolph JT, Wagner R, Collins C.

Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e02558-16. doi: 10.1128/AAC.02558-16. Print 2017 May.

4.

Discovery of fluorobenzimidazole HCV NS5A inhibitors.

Randolph JT, Flentge CA, Donner P, Rockway TW, Patel SV, Nelson L, Hutchinson DK, Mondal R, Mistry N, Reisch T, Dekhtyar T, Krishnan P, Pilot-Matias T, Stolarik DF, Beno DWA, Wagner R, Maring C, Kati WM.

Bioorg Med Chem Lett. 2016 Nov 15;26(22):5462-5467. doi: 10.1016/j.bmcl.2016.10.030. Epub 2016 Oct 13.

PMID:
27780635
5.

Discovery of ABT-267, a pan-genotypic inhibitor of HCV NS5A.

DeGoey DA, Randolph JT, Liu D, Pratt J, Hutchins C, Donner P, Krueger AC, Matulenko M, Patel S, Motter CE, Nelson L, Keddy R, Tufano M, Caspi DD, Krishnan P, Mistry N, Koev G, Reisch TJ, Mondal R, Pilot-Matias T, Gao Y, Beno DW, Maring CJ, Molla A, Dumas E, Campbell A, Williams L, Collins C, Wagner R, Kati WM.

J Med Chem. 2014 Mar 13;57(5):2047-57. doi: 10.1021/jm401398x. Epub 2014 Jan 15.

PMID:
24400777
6.

High potency improvements to weak aryl uracil HCV polymerase inhibitor leads.

Donner P, Randolph JT, Huang P, Wagner R, Maring C, Lim BH, Colletti L, Liu Y, Mondal R, Beyer J, Koev G, Marsh K, Beno D, Longenecker K, Pilot-Matias T, Kati W, Molla A, Kempf D.

Bioorg Med Chem Lett. 2013 Aug 1;23(15):4367-9. doi: 10.1016/j.bmcl.2013.05.078. Epub 2013 Jun 4.

PMID:
23791079
7.

Aryl uracil inhibitors of hepatitis C virus NS5B polymerase: synthesis and characterization of analogs with a fused 5,6-bicyclic ring motif.

Krueger AC, Randolph JT, DeGoey DA, Donner PL, Flentge CA, Hutchinson DK, Liu D, Motter CE, Rockway TW, Wagner R, Beno DW, Koev G, Lim HB, Beyer JM, Mondal R, Liu Y, Kati WM, Longenecker KL, Molla A, Stewart KD, Maring CJ.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3487-90. doi: 10.1016/j.bmcl.2013.04.057. Epub 2013 May 1.

PMID:
23664214
8.

Identification of aryl dihydrouracil derivatives as palm initiation site inhibitors of HCV NS5B polymerase.

Liu Y, Lim BH, Jiang WW, Flentge CA, Hutchinson DK, Madigan DL, Randolph JT, Wagner R, Maring CJ, Kati WM, Molla A.

Bioorg Med Chem Lett. 2012 Jun 1;22(11):3747-50. doi: 10.1016/j.bmcl.2012.04.017. Epub 2012 Apr 10.

PMID:
22542020
9.

Identification of proteasome gene regulation in a rat model for HIV protease inhibitor-induced hyperlipidemia.

Waring JF, Ciurlionis R, Marsh K, Klein LL, Degoey DA, Randolph JT, Spear B, Kempf DJ.

Arch Toxicol. 2010 Apr;84(4):263-70. doi: 10.1007/s00204-010-0527-7. Epub 2010 Mar 6.

PMID:
20213465
10.

Synthesis and evaluation of inhibitors of cytochrome P450 3A (CYP3A) for pharmacokinetic enhancement of drugs.

Flentge CA, Randolph JT, Huang PP, Klein LL, Marsh KC, Harlan JE, Kempf DJ.

Bioorg Med Chem Lett. 2009 Sep 15;19(18):5444-8. doi: 10.1016/j.bmcl.2009.07.118. Epub 2009 Jul 30.

PMID:
19679477
11.

Synthesis and biological characterization of B-ring amino analogues of potent benzothiadiazine hepatitis C virus polymerase inhibitors.

Randolph JT, Flentge CA, Huang PP, Hutchinson DK, Klein LL, Lim HB, Mondal R, Reisch T, Montgomery DA, Jiang WW, Masse SV, Hernandez LE, Henry RF, Liu Y, Koev G, Kati WM, Stewart KD, Beno DW, Molla A, Kempf DJ.

J Med Chem. 2009 May 28;52(10):3174-83. doi: 10.1021/jm801485z.

PMID:
19402666
12.

2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.

Degoey DA, Grampovnik DJ, Flentge CA, Flosi WJ, Chen HJ, Yeung CM, Randolph JT, Klein LL, Dekhtyar T, Colletti L, Marsh KC, Stoll V, Mamo M, Morfitt DC, Nguyen B, Schmidt JM, Swanson SJ, Mo H, Kati WM, Molla A, Kempf DJ.

J Med Chem. 2009 Apr 23;52(8):2571-86. doi: 10.1021/jm900044w.

PMID:
19323562
13.

Synthesis, antiviral activity, and conformational studies of a P3 aza-peptide analog of a potent macrocyclic tripeptide HCV protease inhibitor.

Randolph JT, Zhang X, Huang PP, Klein LL, Kurtz KA, Konstantinidis AK, He W, Kati WM, Kempf DJ.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2745-50. doi: 10.1016/j.bmcl.2008.02.053. Epub 2008 Feb 26.

PMID:
18375121
14.

Pharmacokinetic enhancement of the hepatitis C virus protease inhibitors VX-950 and SCH 503034 by co-dosing with ritonavir.

Kempf DJ, Klein C, Chen HJ, Klein LL, Yeung C, Randolph JT, Lau YY, Chovan LE, Guan Z, Hernandez L, Turner TM, Dandliker PJ, Marsh KC.

Antivir Chem Chemother. 2007;18(3):163-7.

PMID:
17626600
15.

Synthesis, antiviral activity, and pharmacokinetic evaluation of P3 pyridylmethyl analogs of oximinoarylsulfonyl HIV-1 protease inhibitors.

Randolph JT, Huang PP, Flosi WJ, DeGoey D, Klein LL, Yeung CM, Flentge C, Sun M, Zhao C, Dekhtyar T, Mo H, Colletti L, Kati W, Marsh KC, Molla A, Kempf DJ.

Bioorg Med Chem. 2006 Jun 15;14(12):4035-46. Epub 2006 Feb 28.

PMID:
16504523
16.

Practical preclinical model for assessing the potential for unconjugated hyperbilirubinemia produced by human immunodeficiency virus protease inhibitors.

Kempf DJ, Waring JF, Morfitt DC, Werner P, Ebert B, Mitten M, Nguyen B, Randolph JT, DeGoey DA, Klein LL, Marsh K.

Antimicrob Agents Chemother. 2006 Feb;50(2):762-4.

17.

Oximinoarylsulfonamides as potent HIV protease inhibitors.

Yeung CM, Klein LL, Flentge CA, Randolph JT, Zhao C, Sun M, Dekhtyar T, Stoll VS, Kempf DJ.

Bioorg Med Chem Lett. 2005 May 2;15(9):2275-8.

PMID:
15837308
18.

Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors.

Huang PP, Randolph JT, Klein LL, Vasavanonda S, Dekhtyar T, Stoll VS, Kempf DJ.

Bioorg Med Chem Lett. 2004 Aug 2;14(15):4075-8.

PMID:
15225729
19.

Peptidomimetic inhibitors of HIV protease.

Randolph JT, DeGoey DA.

Curr Top Med Chem. 2004;4(10):1079-95. Review.

PMID:
15193140
20.

Mutations conferring resistance to a potent hepatitis C virus serine protease inhibitor in vitro.

Lu L, Pilot-Matias TJ, Stewart KD, Randolph JT, Pithawalla R, He W, Huang PP, Klein LL, Mo H, Molla A.

Antimicrob Agents Chemother. 2004 Jun;48(6):2260-6.

21.

Elimination of antibacterial activities of non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists derived from erythromycin A.

Randolph JT, Sauer DR, Haviv F, Nilius AM, Greer J.

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1599-602.

PMID:
15006412
22.

Nonpeptide luteinizing hormone-releasing hormone antagonists derived from erythromycin A: design, synthesis, and biological activity of cladinose replacement analogues.

Randolph JT, Waid P, Nichols C, Sauer D, Haviv F, Diaz G, Bammert G, Besecke LM, Segreti JA, Mohning KM, Bush EN, Wegner CD, Greer J.

J Med Chem. 2004 Feb 26;47(5):1085-97.

PMID:
14971889
23.

Bacterial lipopolysaccharide has structural similarity to ceramide and stimulates ceramide-activated protein kinase in myeloid cells.

Joseph CK, Wright SD, Bornmann WG, Randolph JT, Kumar ER, Bittman R, Liu J, Kolesnick RN.

J Biol Chem. 1994 Jul 1;269(26):17606-10.

24.

A strategy for the solid-phase synthesis of oligosaccharides.

Danishefsky SJ, McClure KF, Randolph JT, Ruggeri RB.

Science. 1993 May 28;260(5112):1307-9.

PMID:
8493573

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