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Items: 1 to 50 of 53

1.

Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group.

Bungard CJ, Williams PD, Ballard JE, Bennett DJ, Beaulieu C, Bahnck-Teets C, Carroll SS, Chang RK, Dubost DC, Fay JF, Diamond TL, Greshock TJ, Hao L, Holloway MK, Felock PJ, Gesell JJ, Su HP, Manikowski JJ, McKay DJ, Miller M, Min X, Molinaro C, Moradei OM, Nantermet PG, Nadeau C, Sanchez RI, Satyanarayana T, Shipe WD, Singh SK, Truong VL, Vijayasaradhi S, Wiscount CM, Vacca JP, Crane SN, McCauley JA.

ACS Med Chem Lett. 2016 May 9;7(7):702-7. doi: 10.1021/acsmedchemlett.6b00135. eCollection 2016 Jul 14.

2.

Antiviral activity and in vitro mutation development pathways of MK-6186, a novel nonnucleoside reverse transcriptase inhibitor.

Lu M, Felock PJ, Munshi V, Hrin RC, Wang YJ, Yan Y, Munshi S, McGaughey GB, Gomez R, Anthony NJ, Williams TM, Grobler JA, Hazuda DJ, McKenna PM, Miller MD, Lai MT.

Antimicrob Agents Chemother. 2012 Jun;56(6):3324-35. doi: 10.1128/AAC.00102-12. Epub 2012 Mar 5.

3.

Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.

Gomez R, Jolly S, Williams T, Tucker T, Tynebor R, Vacca J, McGaughey G, Lai MT, Felock P, Munshi V, DeStefano D, Touch S, Miller M, Yan Y, Sanchez R, Liang Y, Paton B, Wan BL, Anthony N.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7344-50. doi: 10.1016/j.bmcl.2011.10.027. Epub 2011 Oct 17.

PMID:
22071300
4.

Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.

Gomez R, Jolly SJ, Williams T, Vacca JP, Torrent M, McGaughey G, Lai MT, Felock P, Munshi V, Distefano D, Flynn J, Miller M, Yan Y, Reid J, Sanchez R, Liang Y, Paton B, Wan BL, Anthony N.

J Med Chem. 2011 Nov 24;54(22):7920-33. doi: 10.1021/jm2010173. Epub 2011 Oct 28.

PMID:
21985673
5.

Distinct mutation pathways of non-subtype B HIV-1 during in vitro resistance selection with nonnucleoside reverse transcriptase inhibitors.

Lai MT, Lu M, Felock PJ, Hrin RC, Wang YJ, Yan Y, Munshi S, McGaughey GB, Tynebor RM, Tucker TJ, Williams TM, Grobler JA, Hazuda DJ, McKenna PM, Miller MD.

Antimicrob Agents Chemother. 2010 Nov;54(11):4812-24. doi: 10.1128/AAC.00829-10. Epub 2010 Aug 30.

6.

Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.

Su DS, Lim JJ, Tinney E, Tucker TJ, Saggar S, Sisko JT, Wan BL, Young MB, Anderson KD, Rudd D, Munshi V, Bahnck C, Felock PJ, Lu M, Lai MT, Touch S, Moyer G, Distefano DJ, Flynn JA, Liang Y, Sanchez R, Perlow-Poehnelt R, Miller M, Vacca JP, Williams TM, Anthony NJ.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4328-32. doi: 10.1016/j.bmcl.2010.06.083. Epub 2010 Jun 17.

PMID:
20609585
7.

Triple Hyp→Pro replacement in integramide A, a peptaib inhibitor of HIV-1 integrase: Effect on conformation and bioactivity.

De Zotti M, De Borggraeve W, Kaptein B, Broxterman QB, Singh SB, Felock PJ, Hazuda DJ, Formaggio F, Toniolo C.

Biopolymers. 2011;96(1):49-59. doi: 10.1002/bip.21461.

PMID:
20560143
8.

Assessment of the susceptibility of mutant HIV-1 to antiviral agents.

Wang YJ, McKenna PM, Hrin R, Felock P, Lu M, Jones KG, Coburn CA, Grobler JA, Hazuda DJ, Miller MD, Lai MT.

J Virol Methods. 2010 May;165(2):230-7. doi: 10.1016/j.jviromet.2010.02.002. Epub 2010 Feb 11.

PMID:
20153375
9.

Total synthesis, characterization, and conformational analysis of the naturally occurring hexadecapeptide integramide A and a diastereomer.

De Zotti M, Damato F, Formaggio F, Crisma M, Schievano E, Mammi S, Kaptein B, Broxterman QB, Felock PJ, Hazuda DJ, Singh SB, Kirschbaum J, Brückner H, Toniolo C.

Chemistry. 2010 Jan 4;16(1):316-27. doi: 10.1002/chem.200900945.

PMID:
19937615
10.

Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.

Su DS, Lim JJ, Tinney E, Wan BL, Young MB, Anderson KD, Rudd D, Munshi V, Bahnck C, Felock PJ, Lu M, Lai MT, Touch S, Moyer G, DiStefano DJ, Flynn JA, Liang Y, Sanchez R, Perlow-Poehnelt R, Miller M, Vacca JP, Williams TM, Anthony NJ.

J Med Chem. 2009 Nov 26;52(22):7163-9. doi: 10.1021/jm901230r.

PMID:
19883100
11.

Substituted tetrahydroquinolines as potent allosteric inhibitors of reverse transcriptase and its key mutants.

Su DS, Lim JJ, Tinney E, Wan BL, Young MB, Anderson KD, Rudd D, Munshi V, Bahnck C, Felock PJ, Lu M, Lai MT, Touch S, Moyer G, Distefano DJ, Flynn JA, Liang Y, Sanchez R, Prasad S, Yan Y, Perlow-Poehnelt R, Torrent M, Miller M, Vacca JP, Williams TM, Anthony NJ.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5119-23. doi: 10.1016/j.bmcl.2009.07.031. Epub 2009 Jul 10.

PMID:
19631528
12.

Complete absolute configuration of integramide A, a natural, 16-mer peptide inhibitor of HIV-1 integrase, elucidated by total synthesis.

De Zotti M, Formaggio F, Kaptein B, Broxterman QB, Felock PJ, Hazuda DJ, Singh SB, Brückner H, Toniolo C.

Chembiochem. 2009 Jan 5;10(1):87-90. doi: 10.1002/cbic.200800443. No abstract available.

PMID:
18850604
13.

Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.

Tucker TJ, Sisko JT, Tynebor RM, Williams TM, Felock PJ, Flynn JA, Lai MT, Liang Y, McGaughey G, Liu M, Miller M, Moyer G, Munshi V, Perlow-Poehnelt R, Prasad S, Reid JC, Sanchez R, Torrent M, Vacca JP, Wan BL, Yan Y.

J Med Chem. 2008 Oct 23;51(20):6503-11. doi: 10.1021/jm800856c. Epub 2008 Oct 1.

PMID:
18826204
14.

Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase.

Melamed JY, Egbertson MS, Varga S, Vacca JP, Moyer G, Gabryelski L, Felock PJ, Stillmock KA, Witmer MV, Schleif W, Hazuda DJ, Leonard Y, Jin L, Ellis JD, Young SD.

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5307-10. doi: 10.1016/j.bmcl.2008.08.038. Epub 2008 Aug 14.

PMID:
18774711
15.

10-Hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones: potent, orally bioavailable HIV-1 integrase strand-transfer inhibitors with activity against integrase mutants.

Wiscount CM, Williams PD, Tran LO, Embrey MW, Fisher TE, Sherman V, Homnick CF, Donnette Staas D, Lyle TA, Wai JS, Vacca JP, Wang Z, Felock PJ, Stillmock KA, Witmer MV, Miller MD, Hazuda DJ, Day AM, Gabryelski LJ, Ecto LT, Schleif WA, DiStefano DJ, Kochansky CJ, Anari MR.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4581-3. doi: 10.1016/j.bmcl.2008.07.037. Epub 2008 Jul 15.

PMID:
18657970
16.

The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations.

Tucker TJ, Saggar S, Sisko JT, Tynebor RM, Williams TM, Felock PJ, Flynn JA, Lai MT, Liang Y, McGaughey G, Liu M, Miller M, Moyer G, Munshi V, Perlow-Poehnelt R, Prasad S, Sanchez R, Torrent M, Vacca JP, Wan BL, Yan Y.

Bioorg Med Chem Lett. 2008 May 1;18(9):2959-66. doi: 10.1016/j.bmcl.2008.03.064. Epub 2008 Mar 25.

PMID:
18396399
17.

Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.

Muraglia E, Kinzel O, Gardelli C, Crescenzi B, Donghi M, Ferrara M, Nizi E, Orvieto F, Pescatore G, Laufer R, Gonzalez-Paz O, Di Marco A, Fiore F, Monteagudo E, Fonsi M, Felock PJ, Rowley M, Summa V.

J Med Chem. 2008 Feb 28;51(4):861-74. doi: 10.1021/jm701164t. Epub 2008 Jan 25.

PMID:
18217703
18.

Design and synthesis of substituted 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxamides, novel HIV-1 integrase inhibitors.

Langford HM, Williams PD, Homnick CF, Vacca JP, Felock PJ, Stillmock KA, Witmer MV, Hazuda DJ, Gabryelski LJ, Schleif WA.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):721-5. Epub 2007 Nov 19.

PMID:
18078751
19.

Monitoring the development of non-nucleoside reverse transcriptase inhibitor-associated resistant HIV-1 using an electrochemiluminescence-based reverse transcriptase polymerase assay.

Munshi V, Lu M, Felock P, Barnard RJ, Hazuda DJ, Miller MD, Lai MT.

Anal Biochem. 2008 Mar 1;374(1):121-32. Epub 2007 Oct 9.

PMID:
17964275
20.

8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors.

Fisher TE, Kim B, Staas DD, Lyle TA, Young SD, Vacca JP, Zrada MM, Hazuda DJ, Felock PJ, Schleif WA, Gabryelski LJ, Anari MR, Kochansky CJ, Wai JS.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6511-5. Epub 2007 Sep 29.

PMID:
17931865
21.

Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.

Gardelli C, Nizi E, Muraglia E, Crescenzi B, Ferrara M, Orvieto F, Pace P, Pescatore G, Poma M, Ferreira Mdel R, Scarpelli R, Homnick CF, Ikemoto N, Alfieri A, Verdirame M, Bonelli F, Paz OG, Taliani M, Monteagudo E, Pesci S, Laufer R, Felock P, Stillmock KA, Hazuda D, Rowley M, Summa V.

J Med Chem. 2007 Oct 4;50(20):4953-75. Epub 2007 Sep 8.

PMID:
17824681
22.

Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.

Wai JS, Kim B, Fisher TE, Zhuang L, Embrey MW, Williams PD, Staas DD, Culberson C, Lyle TA, Vacca JP, Hazuda DJ, Felock PJ, Schleif WA, Gabryelski LJ, Jin L, Chen IW, Ellis JD, Mallai R, Young SD.

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5595-9. Epub 2007 Aug 22.

PMID:
17822898
23.

A potent and orally active HIV-1 integrase inhibitor.

Egbertson MS, Moritz HM, Melamed JY, Han W, Perlow DS, Kuo MS, Embrey M, Vacca JP, Zrada MM, Cortes AR, Wallace A, Leonard Y, Hazuda DJ, Miller MD, Felock PJ, Stillmock KA, Witmer MV, Schleif W, Gabryelski LJ, Moyer G, Ellis JD, Jin L, Xu W, Braun MP, Kassahun K, Tsou NN, Young SD.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1392-8. Epub 2006 Dec 3.

PMID:
17194584
24.

A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors.

Guare JP, Wai JS, Gomez RP, Anthony NJ, Jolly SM, Cortes AR, Vacca JP, Felock PJ, Stillmock KA, Schleif WA, Moyer G, Gabryelski LJ, Jin L, Chen IW, Hazuda DJ, Young SD.

Bioorg Med Chem Lett. 2006 Jun 1;16(11):2900-4. Epub 2006 Mar 22.

PMID:
16554152
25.

A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells.

Embrey MW, Wai JS, Funk TW, Homnick CF, Perlow DS, Young SD, Vacca JP, Hazuda DJ, Felock PJ, Stillmock KA, Witmer MV, Moyer G, Schleif WA, Gabryelski LJ, Jin L, Chen IW, Ellis JD, Wong BK, Lin JH, Leonard YM, Tsou NN, Zhuang L.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4550-4.

PMID:
16102965
26.

A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase.

Hazuda DJ, Anthony NJ, Gomez RP, Jolly SM, Wai JS, Zhuang L, Fisher TE, Embrey M, Guare JP Jr, Egbertson MS, Vacca JP, Huff JR, Felock PJ, Witmer MV, Stillmock KA, Danovich R, Grobler J, Miller MD, Espeseth AS, Jin L, Chen IW, Lin JH, Kassahun K, Ellis JD, Wong BK, Xu W, Pearson PG, Schleif WA, Cortese R, Emini E, Summa V, Holloway MK, Young SD.

Proc Natl Acad Sci U S A. 2004 Aug 3;101(31):11233-8. Epub 2004 Jul 26.

27.

Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide.

Herath KB, Jayasuriya H, Bills GF, Polishook JD, Dombrowski AW, Guan Z, Felock PJ, Hazuda DJ, Singh SB.

J Nat Prod. 2004 May;67(5):872-4.

PMID:
15165153
28.

Isolation, structure and HIV-1 integrase inhibitory activity of exophillic acid, a novel fungal metabolite from Exophiala pisciphila.

Ondeyka JG, Zink DL, Dombrowski AW, Polishook JD, Felock PJ, Hazuda DJ, Singh SB.

J Antibiot (Tokyo). 2003 Dec;56(12):1018-23.

29.

Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites.

Singh SB, Jayasuriya H, Dewey R, Polishook JD, Dombrowski AW, Zink DL, Guan Z, Collado J, Platas G, Pelaez F, Felock PJ, Hazuda DJ.

J Ind Microbiol Biotechnol. 2003 Dec;30(12):721-31. Epub 2004 Jan 9.

PMID:
14714192
30.

Chemistry and structure-activity relationship of HIV-1 integrase inhibitor integracide B and related natural products.

Singh SB, Ondeyka JG, Schleif WA, Felock P, Hazuda DJ.

J Nat Prod. 2003 Oct;66(10):1338-44.

PMID:
14575434
31.

Isolation, structure, and HIV-1 integrase inhibitory activity of Cytosporic acid, a fungal metabolite produced by a Cytospora sp.

Jayasuriya H, Guan Z, Polishook JD, Dombrowski AW, Felock PJ, Hazuda DJ, Singh SB.

J Nat Prod. 2003 Apr;66(4):551-3.

PMID:
12713414
32.

Four novel bis-(naphtho-gamma-pyrones) isolated from Fusarium species as inhibitors of HIV-1 integrase.

Singh SB, Zink DL, Bills GF, Teran A, Silverman KC, Lingham RB, Felock P, Hazuda DJ.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):713-7.

PMID:
12639565
33.

Integracides: tetracyclic triterpenoid inhibitors of HIV-1 integrase produced by Fusarium sp.

Singh SB, Zink DL, Dombrowski AW, Polishook JD, Ondeyka JG, Hirshfield J, Felock P, Hazuda DJ.

Bioorg Med Chem. 2003 Apr 3;11(7):1577-82.

PMID:
12628681
34.

Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.

Zhuang L, Wai JS, Embrey MW, Fisher TE, Egbertson MS, Payne LS, Guare JP Jr, Vacca JP, Hazuda DJ, Felock PJ, Wolfe AL, Stillmock KA, Witmer MV, Moyer G, Schleif WA, Gabryelski LJ, Leonard YM, Lynch JJ Jr, Michelson SR, Young SD.

J Med Chem. 2003 Feb 13;46(4):453-6.

PMID:
12570367
35.

Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes.

Grobler JA, Stillmock K, Hu B, Witmer M, Felock P, Espeseth AS, Wolfe A, Egbertson M, Bourgeois M, Melamed J, Wai JS, Young S, Vacca J, Hazuda DJ.

Proc Natl Acad Sci U S A. 2002 May 14;99(10):6661-6. Epub 2002 May 7.

36.

Integramides A and B, two novel non-ribosomal linear peptides containing nine C(alpha)-methyl amino acids produced by fungal fermentations that are inhibitors of HIV-1 integrase.

Singh SB, Herath K, Guan Z, Zink DL, Dombrowski AW, Polishook JD, Silverman KC, Lingham RB, Felock PJ, Hazuda DJ.

Org Lett. 2002 May 2;4(9):1431-4. Erratum in: Org Lett 2002 Sep 19;4(19):3337.

PMID:
11975596
37.

Structure, stereochemistry, and biological activity of integramycin, a novel hexacyclic natural product produced by Actinoplanes sp. that inhibits HIV-1 integrase.

Singh SB, Zink DL, Heimbach B, Genilloud O, Teran A, Silverman KC, Lingham RB, Felock P, Hazuda DJ.

Org Lett. 2002 Apr 4;4(7):1123-6.

PMID:
11922798
38.

The complestatins as HIV-1 integrase inhibitors. Efficient isolation, structure elucidation, and inhibitory activities of isocomplestatin, chloropeptin I, new complestatins, A and B, and acid-hydrolysis products of chloropeptin I.

Singh SB, Jayasuriya H, Salituro GM, Zink DL, Shafiee A, Heimbuch B, Silverman KC, Lingham RB, Genilloud O, Teran A, Vilella D, Felock P, Hazuda D.

J Nat Prod. 2001 Jul;64(7):874-82.

PMID:
11473415
39.

4-Aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells.

Wai JS, Egbertson MS, Payne LS, Fisher TE, Embrey MW, Tran LO, Melamed JY, Langford HM, Guare JP Jr, Zhuang L, Grey VE, Vacca JP, Holloway MK, Naylor-Olsen AM, Hazuda DJ, Felock PJ, Wolfe AL, Stillmock KA, Schleif WA, Gabryelski LJ, Young SD.

J Med Chem. 2000 Dec 28;43(26):4923-6. No abstract available.

PMID:
11150161
40.

HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase.

Espeseth AS, Felock P, Wolfe A, Witmer M, Grobler J, Anthony N, Egbertson M, Melamed JY, Young S, Hamill T, Cole JL, Hazuda DJ.

Proc Natl Acad Sci U S A. 2000 Oct 10;97(21):11244-9.

41.

Chemical and enzymatic modifications of integric acid and HIV-1 integrase inhibitory activity.

Singh SB, Felock P, Hazuda DJ.

Bioorg Med Chem Lett. 2000 Feb 7;10(3):235-8.

PMID:
10698443
42.

X-ray structure of simian immunodeficiency virus integrase containing the core and C-terminal domain (residues 50-293)--an initial glance of the viral DNA binding platform.

Chen Z, Yan Y, Munshi S, Li Y, Zugay-Murphy J, Xu B, Witmer M, Felock P, Wolfe A, Sardana V, Emini EA, Hazuda D, Kuo LC.

J Mol Biol. 2000 Feb 18;296(2):521-33.

PMID:
10669606
43.

Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells.

Hazuda DJ, Felock P, Witmer M, Wolfe A, Stillmock K, Grobler JA, Espeseth A, Gabryelski L, Schleif W, Blau C, Miller MD.

Science. 2000 Jan 28;287(5453):646-50.

44.

Purification, solution properties and crystallization of SIV integrase containing a continuous core and C-terminal domain.

Li Y, Yan Y, Zugay-Murphy J, Xu B, Cole JL, Witmer M, Felock P, Wolfe A, Hazuda D, Sardana MK, Chen Z, Kuo LC, Sardana VV.

Acta Crystallogr D Biol Crystallogr. 1999 Nov;55(Pt 11):1906-10.

PMID:
10531491
45.

Efficiency and fidelity of full-site integration reactions using recombinant simian immunodeficiency virus integrase.

Goodarzi G, Pursley M, Felock P, Witmer M, Hazuda D, Brackmann K, Grandgenett D.

J Virol. 1999 Oct;73(10):8104-11.

46.

Isolation and characterization of novel human immunodeficiency virus integrase inhibitors from fungal metabolites.

Hazuda D, Blau CU, Felock P, Hastings J, Pramanik B, Wolfe A, Bushman F, Farnet C, Goetz M, Williams M, Silverman K, Lingham R, Singh S.

Antivir Chem Chemother. 1999 Mar;10(2):63-70.

PMID:
10335400
47.
48.

Discovery and analysis of inhibitors of the human immunodeficiency integrase.

Hazuda D, Felock PJ, Hastings JC, Pramanik B, Wolfe AL.

Drug Des Discov. 1997 May;15(1):17-24.

PMID:
9332828
49.

Equivalent inhibition of half-site and full-site retroviral strand transfer reactions by structurally diverse compounds.

Hazuda D, Felock P, Hastings J, Pramanik B, Wolfe A, Goodarzi G, Vora A, Brackmann K, Grandgenett D.

J Virol. 1997 Jan;71(1):807-11.

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