S
Stuart W. McCombie
Researcher at Schering-Plough
Publications - 154
Citations - 4885
Stuart W. McCombie is an academic researcher from Schering-Plough. The author has contributed to research in topics: Lactam & Alkylation. The author has an hindex of 29, co-authored 154 publications receiving 4757 citations.
Papers
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Journal ArticleDOI
A new method for the deoxygenation of secondary alcohols
TL;DR: In this paper, a general synthesis of O-cycloalkyl thioesters has been developed which gives access to O-cycle-alkyl seleno-formates and selenobenzoates.
Journal ArticleDOI
SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo.
Julie M. Strizki,Serena Xu,Nicole Wagner,Lisa Wojcik,Jia Liu,Yan Hou,Matthias Endres,Anandan Palani,Sherry Shapiro,John W. Clader,William J. Greenlee,Jayaram R. Tagat,Stuart W. McCombie,Kathleen Cox,Ahmad Fawzi,Chuan-Chu Chou,Catherine Pugliese-Sivo,Liza Davies,Mary E. Moreno,David D. Ho,Alexandra Trkola,Cheryl A. Stoddart,John P. Moore,Gregory R. Reyes,Bahige M. Baroudy +24 more
TL;DR: SCH-C has broad and potent antiviral activity in vitro against primary HIV-1 isolates that use CCR5 as their entry coreceptor, with mean 50% inhibitory concentrations ranging between 0.4 and 9 nM.
Journal ArticleDOI
HIV-1 escape from a small molecule, CCR5-specific entry inhibitor does not involve CXCR4 use
Alexandra Trkola,Shawn E. Kuhmann,Julie M. Strizki,Elizabeth S. Maxwell,Tom Ketas,Thomas Hunt Morgan,Pavel Pugach,Serena Xu,Lisa Wojcik,Jayaram R. Tagat,Anandan Palani,Sherry Shapiro,John W. Clader,Stuart W. McCombie,Gregory R. Reyes,Bahige M. Baroudy,John P. Moore +16 more
TL;DR: HIV-1 acquires the ability to use CCR5 despite the inhibitor, first by requiring lower levels of C CR5 for entry and then probably by using the drug-bound form of the receptor.
Patent
Piperidine derivatives useful as CCR5 antagonists
Bahige M. Baroudy,John W. Clader,Hubert B. Josien,Stuart W. McCombie,Mckittrick Brian A,Michael W. Miller,Bernard R. Neustadt,Anandan Palani,Steensma Ruo,Jayaram R. Tagat,Vice Susan F,Laughlin Mark A +11 more
TL;DR: The use of CCR5 antagonists of formula (I) or a pharmaceutically acceptable salt thereof, wherein X is -C(R13)2-, -C (R13)(R13), R19)-, -c(O)-, O-, -NH-, -N(alkyl)-, (a), (b), (c), (d), (e), (f), (g, (h), (h, (i), (j), (k, (k), (l), (m), (n) or (n
Journal ArticleDOI
Analysis of the Mechanism by Which the Small-Molecule CCR5 Antagonists SCH-351125 and SCH-350581 Inhibit Human Immunodeficiency Virus Type 1 Entry
Fotini Tsamis,Svetlana Gavrilov,Francis Kajumo,Christoph Seibert,Shawn E. Kuhmann,Tom Ketas,Alexandra Trkola,Anadan Palani,John W. Clader,Jayaram R. Tagat,Stuart W. McCombie,Bahige M. Baroudy,John P. Moore,Thomas P. Sakmar,Tatjana Dragic +14 more
TL;DR: The mechanism of action of two inhibitors of CCR5 function are identified, SCH-350581 (AD101) and SCH-351125 (SCH-C), which are more potent than SCH-C at inhibiting HIV-1 replication in primary lymphocytes, as well as viral entry and gp120 binding to cell lines.