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Items: 24

1.

Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold.

Williams PD, Staas DD, Venkatraman S, Loughran HM, Ruzek RD, Booth TM, Lyle TA, Wai JS, Vacca JP, Feuston BP, Ecto LT, Flynn JA, DiStefano DJ, Hazuda DJ, Bahnck CM, Himmelberger AL, Dornadula G, Hrin RC, Stillmock KA, Witmer MV, Miller MD, Grobler JA.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6754-7. doi: 10.1016/j.bmcl.2010.08.135. Epub 2010 Sep 24.

PMID:
20869872
2.

Scintillation proximity assays for mechanistic and pharmacological analyses of HIV-1 integration.

Grobler JA, Stillmock KA, Hazuda DJ.

Methods. 2009 Apr;47(4):249-53. doi: 10.1016/j.ymeth.2009.03.002. Epub 2009 Mar 12.

PMID:
19285556
3.

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
4.

Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.

Summa V, Petrocchi A, Bonelli F, Crescenzi B, Donghi M, Ferrara M, Fiore F, Gardelli C, Gonzalez Paz O, Hazuda DJ, Jones P, Kinzel O, Laufer R, Monteagudo E, Muraglia E, Nizi E, Orvieto F, Pace P, Pescatore G, Scarpelli R, Stillmock K, Witmer MV, Rowley M.

J Med Chem. 2008 Sep 25;51(18):5843-55. doi: 10.1021/jm800245z.

PMID:
18763751
5.

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
6.

Mechanisms of human immunodeficiency virus type 1 concerted integration related to strand transfer inhibition and drug resistance.

Zahm JA, Bera S, Pandey KK, Vora A, Stillmock K, Hazuda D, Grandgenett DP.

Antimicrob Agents Chemother. 2008 Sep;52(9):3358-68. doi: 10.1128/AAC.00271-08. Epub 2008 Jun 30.

7.

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
8.

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
9.

Inhibition of human immunodeficiency virus type 1 concerted integration by strand transfer inhibitors which recognize a transient structural intermediate.

Pandey KK, Bera S, Zahm J, Vora A, Stillmock K, Hazuda D, Grandgenett DP.

J Virol. 2007 Nov;81(22):12189-99. Epub 2007 Sep 5.

10.

Dissecting Tn5 transposition using HIV-1 integrase diketoacid inhibitors.

Czyz A, Stillmock KA, Hazuda DJ, Reznikoff WS.

Biochemistry. 2007 Sep 25;46(38):10776-89. Epub 2007 Aug 29.

PMID:
17725323
11.

Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.

Pace P, Di Francesco ME, Gardelli C, Harper S, Muraglia E, Nizi E, Orvieto F, Petrocchi A, Poma M, Rowley M, Scarpelli R, Laufer R, Gonzalez Paz O, Monteagudo E, Bonelli F, Hazuda D, Stillmock KA, Summa V.

J Med Chem. 2007 May 3;50(9):2225-39. Epub 2007 Apr 12.

PMID:
17428043
12.

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
13.

From dihydroxypyrimidine carboxylic acids to carboxamide HIV-1 integrase inhibitors: SAR around the amide moiety.

Petrocchi A, Koch U, Matassa VG, Pacini B, Stillmock KA, Summa V.

Bioorg Med Chem Lett. 2007 Jan 15;17(2):350-3. Epub 2006 Oct 25.

PMID:
17107799
14.

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
15.

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
16.

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.

17.

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
18.

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.

19.

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
20.

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.

21.

Analysis of the intracellular transport properties of recombinant La Crosse virus glycoproteins.

Bupp K, Stillmock K, González-Scarano F.

Virology. 1996 Jun 15;220(2):485-90.

22.

Protection from La Crosse virus encephalitis with recombinant glycoproteins: role of neutralizing anti-G1 antibodies.

Pekosz A, Griot C, Stillmock K, Nathanson N, Gonzalez-Scarano F.

J Virol. 1995 Jun;69(6):3475-81.

23.

Replication in cultured C2C12 muscle cells correlates with the neuroinvasiveness of California serogroup bunyaviruses.

Griot C, Pekosz A, Davidson R, Stillmock K, Hoek M, Lukac D, Schmeidler D, Cobbinah I, Gonzalez-Scarano F, Nathanson N.

Virology. 1994 Jun;201(2):399-403.

PMID:
8184551
24.

Polygenic control of neuroinvasiveness in California serogroup bunyaviruses.

Griot C, Pekosz A, Lukac D, Scherer SS, Stillmock K, Schmeidler D, Endres MJ, Gonzalez-Scarano F, Nathanson N.

J Virol. 1993 Jul;67(7):3861-7.

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