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PJ Tummino

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Chemicals & Drugs

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Frederick E Boyer; J V N Vara Prasad; John M Domagala; Edmund L Ellsworth; C Gajda; Susan E Hagen; LJ Markoski; Bradley D Tait; Elizabeth A Lunney; A Palovsky; D Ferguson; N Graham; T Holler; DJ Hupe; C Nouhan; PJ Tummino; A Urumov; E Zeikus; G Zeikus; Stephen J Gracheck; J M Sanders; S VanderRoest; Joanne Brodfuehrer; K Iyer; M Sinz; Sergei V Gulnik
5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: potent nonpeptidic inhibitors of HIV protease.
J V N Vara Prasad; Frederick E Boyer; John M Domagala; Edmund L Ellsworth; C Gajda; Harriet W Hamilton; Susan E Hagen; LJ Markoski; B A Steinbaugh; Bradley D Tait; Christine Humblet; Elizabeth A Lunney; Alexander Pavlovsky; John R Rubin; D Ferguson; N Graham; T Holler; DJ Hupe; C Nouhan; PJ Tummino; A Urumov; E Zeikus; G Zeikus; Stephen J Gracheck; John W Erickson
Nonpeptidic HIV protease inhibitors possessing excellent antiviral activities and therapeutic indices. PD 178390: a lead HIV protease inhibitor.
J V N Vara Prasad; LJ Markoski; Frederick E Boyer; John M Domagala; Edmund L Ellsworth; C Gajda; Susan E Hagen; Bradley D Tait; Elizabeth A Lunney; PJ Tummino; D Ferguson; T Holler; DJ Hupe; C Nouhan; Stephen J Gracheck; S VanderRoest; J Saunders; K Iyer; M Sinz
Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety.

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All Publications

2000: Frederick E Boyer; J V N Vara Prasad; John M Domagala; Edmund L Ellsworth; C Gajda; Susan E Hagen; LJ Markoski; Bradley D Tait; Elizabeth A Lunney; A Palovsky; D Ferguson; N Graham; T Holler; DJ Hupe; C Nouhan; PJ Tummino; A Urumov; E Zeikus; G Zeikus; Stephen J Gracheck; J M Sanders; S VanderRoest; Joanne Brodfuehrer; K Iyer; M Sinz; Sergei V Gulnik
5,6-Dihydropyran-2-ones possessing various sulfonyl functionalities: potent nonpeptidic inhibitors of HIV protease.
Journal of medicinal chemistry 2000;43(5):843-58.
1999: J V N Vara Prasad; Frederick E Boyer; John M Domagala; Edmund L Ellsworth; C Gajda; Harriet W Hamilton; Susan E Hagen; LJ Markoski; B A Steinbaugh; Bradley D Tait; Christine Humblet; Elizabeth A Lunney; Alexander Pavlovsky; John R Rubin; D Ferguson; N Graham; T Holler; DJ Hupe; C Nouhan; PJ Tummino; A Urumov; E Zeikus; G Zeikus; Stephen J Gracheck; John W Erickson
Nonpeptidic HIV protease inhibitors possessing excellent antiviral activities and therapeutic indices. PD 178390: a lead HIV protease inhibitor.
Bioorganic & medicinal chemistry 1999;7(12):2775-800.
1999: J V N Vara Prasad; LJ Markoski; Frederick E Boyer; John M Domagala; Edmund L Ellsworth; C Gajda; Susan E Hagen; Bradley D Tait; Elizabeth A Lunney; PJ Tummino; D Ferguson; T Holler; DJ Hupe; C Nouhan; Stephen J Gracheck; S VanderRoest; J Saunders; K Iyer; M Sinz
Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing a novel and achiral 3-(2-t-butyl-5-methyl-4-sulfamate)phenylthio moiety.
Bioorganic & medicinal chemistry letters 1999;9(15):2217-22.
1999: Edmund L Ellsworth; John D Domagala; J V N Vara Prasad; S Hagen; D Ferguson; T Holler; DJ Hupe; N Graham; C Nouhan; PJ Tummino; G Zeikus; Elizabeth A Lunney
4-hydroxy-5,6-dihydro-2H-pyran-2-ones.3. Bicyclic and hetero-aromatic ring systems as 3-position scaffolds to bind to S1' and S2' of the HIV-1 protease enzyme.
Bioorganic & medicinal chemistry letters 1999;9(14):2019-24.
1999: J V N Vara Prasad; Frederick E Boyer; John M Domagala; Edmund L Ellsworth; C Gajda; Susan E Hagen; LJ Markoski; Bradley D Tait; Elizabeth A Lunney; PJ Tummino; D Ferguson; T Holler; DJ Hupe; C Nouhan; Stephen J Gracheck; S VanderRoest; J Saunders; K Iyer; M Sinz; Joanne Brodfuehrer
Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl,5-methylphenyl thio) moiety: antiviral activities and pharmacokinetic properties.
Bioorganic & medicinal chemistry letters 1999;9(11):1481-6.
1997: Bradley D Tait; S Hagen; John D Domagala; Edmund L Ellsworth; C Gajda; Harriet W Hamilton; J V N Vara Prasad; D Ferguson; N Graham; DJ Hupe; C Nouhan; PJ Tummino; Christine Humblet; Elizabeth A Lunney; Alexander Pavlovsky; J Rubin; Stephen J Gracheck; Eric Baldwin; TN Bhat; John W Erickson; Sergei V Gulnik; B Liu
4-hydroxy-5,6-dihydropyrones. 2. Potent non-peptide inhibitors of HIV protease.
Journal of medicinal chemistry 1997;40(23):3781-92.
1997: Susan E Hagen; J V N Vara Prasad; Frederick E Boyer; John M Domagala; Edmund L Ellsworth; C Gajda; Harriet W Hamilton; LJ Markoski; B A Steinbaugh; Bradley D Tait; Elizabeth A Lunney; PJ Tummino; D Ferguson; DJ Hupe; C Nouhan; Stephen J Gracheck; J M Saunders; S VanderRoest
Synthesis of 5,6-dihydro-4-hydroxy-2-pyrones as HIV-1 protease inhibitors: the profound effect of polarity on antiviral activity.
Journal of medicinal chemistry 1997;40(23):3707-11.
1997: John M Domagala; RD Gogliotti; Joseph P Sanchez; Michael A Stier; K Musa; Y Song; Joseph A Loo; M Reily; PJ Tummino; P Harvey; DJ Hupe; L Sharmeen; D Mack; JD Scholten; J Saunders; T McQuade
2,2'-Dithiobisbenzamides and 2-benzisothiazolones, two new classes of antiretroviral agents: SAR and mechanistic considerations.
Drug design and discovery 1997;15(1):49-61.
1997: John M Domagala; JP Bader; RD Gogliotti; Joseph P Sanchez; Michael A Stier; Y Song; J V N Vara Prasad; PJ Tummino; JD Scholten; P Harvey; T Holler; Stephen J Gracheck; DJ Hupe; William G Rice; R Schultz
A new class of anti-HIV-1 agents targeted toward the nucleocapsid protein NCp7: the 2,2'-dithiobisbenzamides.
Bioorganic & medicinal chemistry 1997;5(3):569-79.
1997: PJ Tummino; P J Harvey; T McQuade; John D Domagala; RD Gogliotti; J Sanchez; Y Song; DJ Hupe
The human immunodeficiency virus type 1 (HIV-1) nucleocapsid protein zinc ejection activity of disulfide benzamides and benzisothiazolones: correlation with anti-HIV and virucidal activities.
Antimicrobial agents and chemotherapy 1997;41(2):394-400.
1996: PJ Tummino; J V N Vara Prasad; D Ferguson; C Nouhan; N Graham; J M Domagala; Edmund L Ellsworth; C Gajda; Susan E Hagen; Elizabeth A Lunney; K S Para; Bradley D Tait; Alexander Pavlovsky; John W Erickson; Stephen J Gracheck; T J McQuade; D J Hupe
Discovery and optimization of nonpeptide HIV-1 protease inhibitors.
Bioorganic & medicinal chemistry 1996;4(9):1401-10.
1996: J V N Vara Prasad; PJ Tummino; D Ferguson; J Saunders; S Vander Roest; T J McQuade; A Heldsinger; E L Reyner; B H Stewart; R J Guttendorf; K S Para; Elizabeth A Lunney; Stephen J Gracheck; J M Domagala
Nonpeptidic HIV protease inhibitors: 4-hydroxy-pyran-2-one inhibitors with functional tethers to P1 phenyl ring to reach S3 pocket of the enzyme.
Biochemical and biophysical research communications 1996;221(3):815-20.
1996: J V N Vara Prasad; Elizabeth A Lunney; K S Para; PJ Tummino; D Ferguson; D Hupe; J M Domagala; John W Erickson
Nonpeptidic potent HIV-1 protease inhibitors.
Drug design and discovery 1996;13(3-4):15-28.
1996: Bradley D Tait; J Domagala; Edmund L Ellsworth; D Ferguson; C Gajda; D Hupe; Elizabeth A Lunney; PJ Tummino
Inhibitors of HIV protease: unique non-peptide active site templates.
Journal of molecular recognition : JMR 1996;9(2):139-42.
1996: PJ Tummino; Jeffrey D Scholten; P J Harvey; T Holler; L Maloney; RD Gogliotti; J Domagala; D Hupe
The in vitro ejection of zinc from human immunodeficiency virus (HIV) type 1 nucleocapsid protein by disulfide benzamides with cellular anti-HIV activity.
Proceedings of the National Academy of Sciences of the United States of America 1996;93(3):969-73.
1995: J V N Vara Prasad; K S Para; PJ Tummino; D Ferguson; T J McQuade; Elizabeth A Lunney; Stephen T Rapundalo; BL Batley; G Hingorani; J M Domagala
Nonpeptidic potent HIV-1 protease inhibitors: (4-hydroxy-6-phenyl-2-oxo-2H- pyran-3-yl)thiomethanes that span P1-P2' subsites in a unique mode of active site binding.
Journal of medicinal chemistry 1995;38(6):898-905.
1995: PJ Tummino; D Ferguson; C M Jacobs; B Tait; L Hupe; Elizabeth A Lunney; D Hupe
Competitive inhibition of HIV-1 protease by biphenyl carboxylic acids.
Archives of biochemistry and biophysics 1995;316(1):523-8.
1994: PJ Tummino; D Ferguson; D Hupe
Competitive inhibition of HIV-1 protease by warfarin derivatives.
Biochemical and biophysical research communications 1994;201(1):290-4.
1994: PJ Tummino; D Ferguson; L Hupe; D Hupe
Competitive inhibition of HIV-1 protease by 4-hydroxy-benzopyran-2-ones and by 4-hydroxy-6-phenylpyran-2-ones.
Biochemical and biophysical research communications 1994;200(3):1658-64.