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Items: 49

1.

Preclinical Profile of AB-423, an Inhibitor of Hepatitis B Virus Pregenomic RNA Encapsidation.

Mani N, Cole AG, Phelps JR, Ardzinski A, Cobarrubias KD, Cuconati A, Dorsey BD, Evangelista E, Fan K, Guo F, Guo H, Guo JT, Harasym TO, Kadhim S, Kultgen SG, Lee ACH, Li AHL, Long Q, Majeski SA, Mao R, McClintock KD, Reid SP, Rijnbrand R, Snead NM, Micolochick Steuer HM, Stever K, Tang S, Wang X, Zhao Q, Sofia MJ.

Antimicrob Agents Chemother. 2018 May 25;62(6). pii: e00082-18. doi: 10.1128/AAC.00082-18. Print 2018 Jun.

2.

Combined inhibition of atypical PKC and histone deacetylase 1 is cooperative in basal cell carcinoma treatment.

Mirza AN, Fry MA, Urman NM, Atwood SX, Roffey J, Ott GR, Chen B, Lee A, Brown AS, Aasi SZ, Hollmig T, Ator MA, Dorsey BD, Ruggeri BR, Zificsak CA, Sirota M, Tang JY, Butte A, Epstein E, Sarin KY, Oro AE.

JCI Insight. 2017 Nov 2;2(21). pii: 97071. doi: 10.1172/jci.insight.97071.

3.

Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).

Ott GR, Cheng M, Learn KS, Wagner J, Gingrich DE, Lisko JG, Curry M, Mesaros EF, Ghose AK, Quail MR, Wan W, Lu L, Dobrzanski P, Albom MS, Angeles TS, Wells-Knecht K, Huang Z, Aimone LD, Bruckheimer E, Anderson N, Friedman J, Fernandez SV, Ator MA, Ruggeri BA, Dorsey BD.

J Med Chem. 2016 Aug 25;59(16):7478-96. doi: 10.1021/acs.jmedchem.6b00487. Epub 2016 Aug 15.

PMID:
27527804
4.

Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.

Mesaros EF, Angeles TS, Albom MS, Wagner JC, Aimone LD, Wan W, Lu L, Huang Z, Olsen M, Kordwitz E, Haltiwanger RC, Landis AJ, Cheng M, Ruggeri BA, Ator MA, Dorsey BD, Ott GR.

Bioorg Med Chem Lett. 2015 Mar 1;25(5):1047-52. doi: 10.1016/j.bmcl.2015.01.019. Epub 2015 Jan 17.

PMID:
25655723
5.

Design, synthesis, and biological evaluation of sulfonyl acrylonitriles as novel inhibitors of cancer metastasis and spread.

Shen Y, Zificsak CA, Shea JE, Lao X, Bollt O, Li X, Lisko JG, Theroff JP, Scaife CL, Ator MA, Ruggeri BA, Dorsey BD, Kuwada SK.

J Med Chem. 2015 Feb 12;58(3):1140-58. doi: 10.1021/jm501437v. Epub 2015 Jan 26.

PMID:
25581261
6.

Anaplastic lymphoma kinase inhibitors as anticancer therapeutics: a patent review.

Mesaros EF, Ott GR, Dorsey BD.

Expert Opin Ther Pat. 2014 Apr;24(4):417-42. doi: 10.1517/13543776.2014.877890. Epub 2014 Jan 30. Review.

PMID:
24476492
7.

A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779.

Dugan BJ, Gingrich DE, Mesaros EF, Milkiewicz KL, Curry MA, Zulli AL, Dobrzanski P, Serdikoff C, Jan M, Angeles TS, Albom MS, Mason JL, Aimone LD, Meyer SL, Huang Z, Wells-Knecht KJ, Ator MA, Ruggeri BA, Dorsey BD.

J Med Chem. 2012 Jun 14;55(11):5243-54. doi: 10.1021/jm300248q. Epub 2012 May 18.

PMID:
22594690
8.

Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.

Gingrich DE, Lisko JG, Curry MA, Cheng M, Quail M, Lu L, Wan W, Albom MS, Angeles TS, Aimone LD, Haltiwanger RC, Wells-Knecht K, Ott GR, Ghose AK, Ator MA, Ruggeri B, Dorsey BD.

J Med Chem. 2012 May 24;55(10):4580-93. doi: 10.1021/jm201550q. Epub 2012 May 7.

PMID:
22564207
9.

Synthesis and biological evaluation of sulfonyl acrylonitriles as novel inhibitors to peritoneal carcinomatosis.

Zificsak CA, Shen Y, Lisko JG, Theroff JP, Lao X, Bollt O, Li X, Dorsey BD, Kuwada SK.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1850-3. doi: 10.1016/j.bmcl.2012.01.085. Epub 2012 Jan 30.

PMID:
22326395
10.

CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity.

James J, Ruggeri B, Armstrong RC, Rowbottom MW, Jones-Bolin S, Gunawardane RN, Dobrzanski P, Gardner MF, Zhao H, Cramer MD, Hunter K, Nepomuceno RR, Cheng M, Gitnick D, Yazdanian M, Insko DE, Ator MA, Apuy JL, Faraoni R, Dorsey BD, Williams M, Bhagwat SS, Holladay MW.

Mol Cancer Ther. 2012 Apr;11(4):930-41. doi: 10.1158/1535-7163.MCT-11-0645. Epub 2012 Feb 7.

11.

Knowledge-Based, Central Nervous System (CNS) Lead Selection and Lead Optimization for CNS Drug Discovery.

Ghose AK, Herbertz T, Hudkins RL, Dorsey BD, Mallamo JP.

ACS Chem Neurosci. 2012 Jan 18;3(1):50-68. Epub 2011 Nov 2.

12.

CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers.

Cheng M, Quail MR, Gingrich DE, Ott GR, Lu L, Wan W, Albom MS, Angeles TS, Aimone LD, Cristofani F, Machiorlatti R, Abele C, Ator MA, Dorsey BD, Inghirami G, Ruggeri BA.

Mol Cancer Ther. 2012 Mar;11(3):670-9. doi: 10.1158/1535-7163.MCT-11-0776. Epub 2011 Dec 27.

13.

Design, synthesis, and anaplastic lymphoma kinase (ALK) inhibitory activity for a novel series of 2,4,8,22-tetraazatetracyclo[14.3.1.1³,⁷.1⁹,¹³]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene macrocycles.

Breslin HJ, Lane BM, Ott GR, Ghose AK, Angeles TS, Albom MS, Cheng M, Wan W, Haltiwanger RC, Wells-Knecht KJ, Dorsey BD.

J Med Chem. 2012 Jan 12;55(1):449-64. doi: 10.1021/jm201333e. Epub 2011 Dec 15.

PMID:
22172029
14.

Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.

Zificsak CA, Gingrich DE, Breslin HJ, Dunn DD, Milkiewicz KL, Theroff JP, Thieu TV, Underiner TL, Weinberg LR, Aimone LD, Albom MS, Mason JL, Saville L, Husten J, Angeles TS, Finn JP, Jan M, O'Kane TM, Dobrzanski P, Dorsey BD.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):133-7. doi: 10.1016/j.bmcl.2011.11.049. Epub 2011 Nov 25.

PMID:
22169263
15.

Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.

Rowbottom MW, Faraoni R, Chao Q, Campbell BT, Lai AG, Setti E, Ezawa M, Sprankle KG, Abraham S, Tran L, Struss B, Gibney M, Armstrong RC, Gunawardane RN, Nepomuceno RR, Valenta I, Hua H, Gardner MF, Cramer MD, Gitnick D, Insko DE, Apuy JL, Jones-Bolin S, Ghose AK, Herbertz T, Ator MA, Dorsey BD, Ruggeri B, Williams M, Bhagwat S, James J, Holladay MW.

J Med Chem. 2012 Feb 9;55(3):1082-105. doi: 10.1021/jm2009925. Epub 2012 Jan 23.

PMID:
22168626
16.

Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazines: identification of orally bioavailable, efficacious ALK inhibitors.

Mesaros EF, Thieu TV, Wells GJ, Zificsak CA, Wagner JC, Breslin HJ, Tripathy R, Diebold JL, McHugh RJ, Wohler AT, Quail MR, Wan W, Lu L, Huang Z, Albom MS, Angeles TS, Wells-Knecht KJ, Aimone LD, Cheng M, Ator MA, Ott GR, Dorsey BD.

J Med Chem. 2012 Jan 12;55(1):115-25. doi: 10.1021/jm2010767. Epub 2011 Dec 29.

PMID:
22141319
17.

Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: control of selectivity by a benzyloxy group.

Tripathy R, McHugh RJ, Ghose AK, Ott GR, Angeles TS, Albom MS, Huang Z, Aimone LD, Cheng M, Dorsey BD.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7261-4. doi: 10.1016/j.bmcl.2011.10.055. Epub 2011 Oct 20.

PMID:
22061645
18.

2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation.

Weinberg LR, Albom MS, Angeles TS, Breslin HJ, Gingrich DE, Huang Z, Lisko JG, Mason JL, Milkiewicz KL, Thieu TV, Underiner TL, Wells GJ, Wells-Knecht KJ, Dorsey BD.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7325-30. doi: 10.1016/j.bmcl.2011.10.032. Epub 2011 Oct 14.

PMID:
22041060
19.

2,7-Disubstituted-pyrrolotriazine kinase inhibitors with an unusually high degree of reactive metabolite formation.

Wells-Knecht KJ, Ott GR, Cheng M, Wells GJ, Breslin HJ, Gingrich DE, Weinberg L, Mesaros EF, Huang Z, Yazdanian M, Ator MA, Aimone LD, Zeigler K, Dorsey BD.

Chem Res Toxicol. 2011 Nov 21;24(11):1994-2003. doi: 10.1021/tx200304r. Epub 2011 Nov 4.

PMID:
22023349
20.

Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group.

Milkiewicz KL, Aimone LD, Albom MS, Angeles TS, Chang H, Grobelny JV, Husten J, Losardo C, Miknyoczki S, Murthy S, Rolon-Steele D, Underiner TL, Weinberg LR, Worrell CS, Zeigler KS, Dorsey BD.

Bioorg Med Chem. 2011 Nov 1;19(21):6274-84. doi: 10.1016/j.bmc.2011.09.006. Epub 2011 Sep 13.

PMID:
21967808
21.

Depletion of autoreactive plasma cells and treatment of lupus nephritis in mice using CEP-33779, a novel, orally active, selective inhibitor of JAK2.

Lu LD, Stump KL, Wallace NH, Dobrzanski P, Serdikoff C, Gingrich DE, Dugan BJ, Angeles TS, Albom MS, Mason JL, Ator MA, Dorsey BD, Ruggeri BA, Seavey MM.

J Immunol. 2011 Oct 1;187(7):3840-53. doi: 10.4049/jimmunol.1101228. Epub 2011 Aug 31.

22.

2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazines: new variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity.

Ott GR, Wells GJ, Thieu TV, Quail MR, Lisko JG, Mesaros EF, Gingrich DE, Ghose AK, Wan W, Lu L, Cheng M, Albom MS, Angeles TS, Huang Z, Aimone LD, Ator MA, Ruggeri BA, Dorsey BD.

J Med Chem. 2011 Sep 22;54(18):6328-41. doi: 10.1021/jm200758k. Epub 2011 Aug 22.

PMID:
21859094
23.

4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.

Holladay MW, Campbell BT, Rowbottom MW, Chao Q, Sprankle KG, Lai AG, Abraham S, Setti E, Faraoni R, Tran L, Armstrong RC, Gunawardane RN, Gardner MF, Cramer MD, Gitnick D, Ator MA, Dorsey BD, Ruggeri BR, Williams M, Bhagwat SS, James J.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5342-6. doi: 10.1016/j.bmcl.2011.07.019. Epub 2011 Jul 14.

PMID:
21807507
24.

Discovery and process synthesis of novel 2,7-pyrrolo[2,1-f][1,2,4]triazines.

Thieu T, Sclafani JA, Levy DV, McLean A, Breslin HJ, Ott GR, Bakale RP, Dorsey BD.

Org Lett. 2011 Aug 19;13(16):4204-7. doi: 10.1021/ol2015237. Epub 2011 Jul 26.

PMID:
21790122
25.

Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors.

Zificsak CA, Theroff JP, Aimone LD, Angeles TS, Albom MS, Cheng M, Mesaros EF, Ott GR, Quail MR, Underiner TL, Wan W, Dorsey BD.

Bioorg Med Chem Lett. 2011 Jul 1;21(13):3877-80. doi: 10.1016/j.bmcl.2011.05.040. Epub 2011 May 18.

PMID:
21632243
26.

A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis.

Stump KL, Lu LD, Dobrzanski P, Serdikoff C, Gingrich DE, Dugan BJ, Angeles TS, Albom MS, Ator MA, Dorsey BD, Ruggeri BA, Seavey MM.

Arthritis Res Ther. 2011 Apr 21;13(2):R68. doi: 10.1186/ar3329.

27.

P3 optimization of functional potency, in vivo efficacy and oral bioavailability in 3-aminopyrazinone thrombin inhibitors bearing non-charged groups at the P1 position.

Isaacs RC, Newton CL, Cutrona KJ, Mercer SP, Dorsey BD, McDonough CM, Cook JJ, Krueger JA, Lewis SD, Lucas BJ, Lyle EA, Lynch JJ, Miller-Stein C, Michener MT, Wallace AA, White RB, Wong BK.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1532-5. doi: 10.1016/j.bmcl.2010.12.108. Epub 2010 Dec 28.

PMID:
21295466
28.

2,4-Diaminopyrimidine inhibitors of c-Met kinase bearing benzoxazepine anilines.

Zificsak CA, Theroff JP, Aimone LD, Albom MS, Angeles TS, Brown RA, Galinis D, Grobelny JV, Herbertz T, Husten J, Kocsis LS, LoSardo C, Miknyoczki SJ, Murthy S, Rolon-Steele D, Underiner TL, Wells-Knecht KJ, Worrell CS, Zeigler KS, Dorsey BD.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):660-3. doi: 10.1016/j.bmcl.2010.12.013. Epub 2010 Dec 8.

PMID:
21190849
29.

Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity.

Ott GR, Tripathy R, Cheng M, McHugh R, Anzalone AV, Underiner TL, Curry MA, Quail MR, Lu L, Wan W, Angeles TS, Albom MS, Aimone LD, Ator MA, Ruggeri BA, Dorsey BD.

ACS Med Chem Lett. 2010 Sep 1;1(9):493-8. doi: 10.1021/ml100158s. eCollection 2010 Dec 9.

30.

Synthesis and pharmacological evaluation of N-(3-(1H-indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent.

Shetty RS, Lee Y, Liu B, Husain A, Joseph RW, Lu Y, Nelson D, Mihelcic J, Chao W, Moffett KK, Schumacher A, Flubacher D, Stojanovic A, Bukhtiyarova M, Williams K, Lee KJ, Ochman AR, Saporito MS, Moore WR, Flynn GA, Dorsey BD, Springman EB, Fujimoto T, Kelly MJ.

J Med Chem. 2011 Jan 13;54(1):179-200. doi: 10.1021/jm100659v. Epub 2010 Dec 2.

PMID:
21126027
31.

Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors.

Weinberg LR, Albom MS, Angeles TS, Husten J, Lisko JG, McHugh RJ, Milkiewicz KL, Murthy S, Ott GR, Theroff JP, Tripathy R, Underiner TL, Zificsak CA, Dorsey BD.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):164-7. doi: 10.1016/j.bmcl.2010.11.045. Epub 2010 Nov 11.

PMID:
21123062
32.

Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.

Mesaros EF, Burke JP, Parrish JD, Dugan BJ, Anzalone AV, Angeles TS, Albom MS, Aimone LD, Quail MR, Wan W, Lu L, Huang Z, Ator MA, Ruggeri BA, Cheng M, Ott GR, Dorsey BD.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):463-6. doi: 10.1016/j.bmcl.2010.10.115. Epub 2010 Oct 27. Erratum in: Bioorg Med Chem Lett. 2011 Mar 15;21(6):1900.

PMID:
21074994
33.

Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1.

Liu B, Lee Y, Zou J, Petrassi HM, Joseph RW, Chao W, Michelotti EL, Bukhtiyarova M, Springman EB, Dorsey BD.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6592-6. doi: 10.1016/j.bmcl.2010.09.034. Epub 2010 Sep 21.

PMID:
20888224
34.

Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.

Milkiewicz KL, Weinberg LR, Albom MS, Angeles TS, Cheng M, Ghose AK, Roemmele RC, Theroff JP, Underiner TL, Zificsak CA, Dorsey BD.

Bioorg Med Chem. 2010 Jun 15;18(12):4351-62. doi: 10.1016/j.bmc.2010.04.087. Epub 2010 Apr 29.

PMID:
20483621
35.

Structure-based design of substituted biphenyl ethylene ethers as ligands binding in the hydrophobic pocket of gp41 and blocking the helical bundle formation.

Liu B, Joseph RW, Dorsey BD, Schiksnis RA, Northrop K, Bukhtiyarova M, Springman EB.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5693-7. doi: 10.1016/j.bmcl.2009.08.018. Epub 2009 Aug 8.

PMID:
19699090
36.

Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.

Dorsey BD, Iqbal M, Chatterjee S, Menta E, Bernardini R, Bernareggi A, Cassarà PG, D'Arasmo G, Ferretti E, De Munari S, Oliva A, Pezzoni G, Allievi C, Strepponi I, Ruggeri B, Ator MA, Williams M, Mallamo JP.

J Med Chem. 2008 Feb 28;51(4):1068-72. doi: 10.1021/jm7010589. Epub 2008 Feb 5.

PMID:
18247547
37.

Anaplastic lymphoma kinase activity is essential for the proliferation and survival of anaplastic large-cell lymphoma cells.

Wan W, Albom MS, Lu L, Quail MR, Becknell NC, Weinberg LR, Reddy DR, Holskin BP, Angeles TS, Underiner TL, Meyer SL, Hudkins RL, Dorsey BD, Ator MA, Ruggeri BA, Cheng M.

Blood. 2006 Feb 15;107(4):1617-23. Epub 2005 Oct 27.

38.

Benzodiazepines as potent and selective bradykinin B1 antagonists.

Wood MR, Kim JJ, Han W, Dorsey BD, Homnick CF, DiPardo RM, Kuduk SD, MacNeil T, Murphy KL, Lis EV, Ransom RW, Stump GL, Lynch JJ, O'Malley SS, Miller PJ, Chen TB, Harrell CM, Chang RS, Sandhu P, Ellis JD, Bondiskey PJ, Pettibone DJ, Freidinger RM, Bock MG.

J Med Chem. 2003 May 8;46(10):1803-6.

PMID:
12723943
39.

Azaindoles: moderately basic P1 groups for enhancing the selectivity of thrombin inhibitors.

Sanderson PE, Stanton MG, Dorsey BD, Lyle TA, McDonough C, Sanders WM, Savage KL, Naylor-Olsen AM, Krueger JA, Lewis SD, Lucas BJ, Lynch JJ, Yan Y.

Bioorg Med Chem Lett. 2003 Mar 10;13(5):795-8.

PMID:
12617893
40.

Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines.

Burgey CS, Robinson KA, Lyle TA, Sanderson PE, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Williams PD, Coburn CA, Dorsey BD, Barrow JC, Stranieri MT, Holahan MA, Sitko GR, Cook JJ, McMasters DR, McDonough CM, Sanders WM, Wallace AA, Clayton FC, Bohn D, Leonard YM, Detwiler TJ Jr, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP.

J Med Chem. 2003 Feb 13;46(4):461-73.

PMID:
12570369
41.

Identification of MK-944a: a second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors.

Dorsey BD, McDonough C, McDaniel SL, Levin RB, Newton CL, Hoffman JM, Darke PL, Zugay-Murphy JA, Emini EA, Schleif WA, Olsen DB, Stahlhut MW, Rutkowski CA, Kuo LC, Lin JH, Chen IW, Michelson SR, Holloway MK, Huff JR, Vacca JP.

J Med Chem. 2000 Sep 7;43(18):3386-99.

PMID:
10978186
42.

L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.

Sanderson PE, Cutrona KJ, Dorsey BD, Dyer DL, McDonough CM, Naylor-Olsen AM, Chen IW, Chen Z, Cook JJ, Gardell SJ, Krueger JA, Lewis SD, Lin JH, Lucas BJ Jr, Lyle EA, Lynch JJ Jr, Stranieri MT, Vastag K, Shafer JA, Vacca JP.

Bioorg Med Chem Lett. 1998 Apr 7;8(7):817-22.

PMID:
9871547
43.

Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.

Sanderson PE, Lyle TA, Cutrona KJ, Dyer DL, Dorsey BD, McDonough CM, Naylor-Olsen AM, Chen IW, Chen Z, Cook JJ, Cooper CM, Gardell SJ, Hare TR, Krueger JA, Lewis SD, Lin JH, Lucas BJ Jr, Lyle EA, Lynch JJ Jr, Stranieri MT, Vastag K, Yan Y, Shafer JA, Vacca JP.

J Med Chem. 1998 Nov 5;41(23):4466-74.

PMID:
9804686
44.

Metabolite-P450 complex formation by methylenedioxyphenyl HIV protease inhibitors in rat and human liver microsomes.

Chiba M, Nishime JA, Chen IW, Vastag KJ, Sahly YS, Kim BM, Dorsey BD, Vacca JP, Lin JH.

Biochem Pharmacol. 1998 Jul 15;56(2):223-30.

PMID:
9698076
45.

Time- and dose-dependent pharmacokinetics of L-754,394, an HIV protease inhibitor, in rats, dogs and monkeys.

Lin JH, Chiba M, Chen IW, Vastag KJ, Nishime JA, Dorsey BD, Michelson SR, McDaniel SL.

J Pharmacol Exp Ther. 1995 Jul;274(1):264-9.

PMID:
7616407
46.

A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site.

Holloway MK, Wai JM, Halgren TA, Fitzgerald PM, Vacca JP, Dorsey BD, Levin RB, Thompson WJ, Chen LJ, deSolms SJ.

J Med Chem. 1995 Jan 20;38(2):305-17. Erratum in: J Med Chem 1996 May 24;39(11):2280.

PMID:
7830273
47.

L-735,524: the design of a potent and orally bioavailable HIV protease inhibitor.

Dorsey BD, Levin RB, McDaniel SL, Vacca JP, Guare JP, Darke PL, Zugay JA, Emini EA, Schleif WA, Quintero JC, et al.

J Med Chem. 1994 Oct 14;37(21):3443-51.

PMID:
7932573
48.

Synthesis, antiviral activity, and bioavailability studies of gamma-lactam derived HIV protease inhibitors.

Hungate RW, Chen JL, Starbuck KE, Vacca JP, McDaniel SL, Levin RB, Dorsey BD, Guare JP, Holloway MK, Whitter W, et al.

Bioorg Med Chem. 1994 Sep;2(9):859-79.

PMID:
7712123
49.

L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor.

Vacca JP, Dorsey BD, Schleif WA, Levin RB, McDaniel SL, Darke PL, Zugay J, Quintero JC, Blahy OM, Roth E, et al.

Proc Natl Acad Sci U S A. 1994 Apr 26;91(9):4096-100.

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