Madelene Antane
Princeton University
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Publication
Featured researches published by Madelene Antane.
Journal of Medicinal Chemistry | 2008
Scott Christian Mayer; Anthony F. Kreft; Boyd L. Harrison; Magid Abou-Gharbia; Madelene Antane; Suzan Aschmies; Kevin Atchison; Michael Chlenov; Derek Cecil Cole; Thomas A. Comery; George Diamantidis; John W. Ellingboe; Kristi Fan; Rocco John Galante; Cathleen Gonzales; Douglas M. Ho; Molly Hoke; Yun Hu; Donna M. Huryn; Uday Jain; Mei Jin; Kenneth Alfred Martin Kremer; Dennis M. Kubrak; Melissa Lin; Peimin Lu; Ron Magolda; Robert Martone; William M. Moore; Aram Oganesian; Menelas N. Pangalos
SAR on HTS hits 1 and 2 led to the potent, Notch-1-sparing GSI 9, which lowered brain Abeta in Tg2576 mice at 100 mg/kg po. Converting the metabolically labile methyl groups in 9 to trifluoromethyl groups afforded the more stable analogue 10, which had improved in vivo potency. Further side chain modification afforded the potent Notch-1-sparing GSI begacestat (5), which was selected for development for the treatment of Alzheimers disease.
Bioorganic & Medicinal Chemistry Letters | 2009
Derek Cecil Cole; Joseph Raymond Stock; Anthony F. Kreft; Madelene Antane; Suzan Aschmies; Kevin Atchison; David S. Casebier; Thomas A. Comery; George Diamantidis; John W. Ellingboe; Boyd L. Harrison; Yun Hu; Mei Jin; Dennis M. Kubrak; Peimin Lu; Charles William Mann; Robert Martone; William Jay Moore; Aram Oganesian; David Riddell; June Sonnenberg-Reines; Shaiu-Ching Sun; Erik Wagner; Zheng Wang; Kevin R. Woller; Zheng Xu; Hua Zhou; J. Steven Jacobsen
Accumulation of beta-amyloid (Abeta), produced by the proteolytic cleavage of amyloid precursor protein (APP) by beta- and gamma-secretase, is widely believed to be associated with Alzheimers disease (AD). Research around the high-throughput screening hit (S)-4-chlorophenylsulfonyl isoleucinol led to the identification of the Notch-1-sparing (9.5-fold) gamma-secretase inhibitor (S)-N-(5-chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol 7.b.2 (Abeta(40/42) EC(50)=28 nM), which is efficacious in reduction of Abeta production in vivo.
Journal of Medicinal Chemistry | 2000
John A. Butera; Madelene Antane; Schuyler Adam Antane; Thomas M. Argentieri; Chris Freeden; Russell Graceffa; Bradford H. Hirth; Douglas John Jenkins; Joseph R. Lennox; Edward Martin Matelan; N. Wesley Norton; Dominick Anthony Quagliato; Jeffrey H. Sheldon; Walter Spinelli; Dawn Warga; and Alexandra Wojdan; Morgan Woods
Journal of Medicinal Chemistry | 2000
Adam M. Gilbert; Madelene Antane; Thomas M. Argentieri; John A. Butera; Gerardo D. Francisco; Chris Freeden; Eric G. Gundersen; Russell Graceffa; David R. Herbst; Bradford H. Hirth; Joseph R. Lennox; Geraldine Ruth Mcfarlane; N. Wesley Norton; Dominick Anthony Quagliato; Jeffrey H. Sheldon; Dawn Warga; and Alexandra Wojdan; Morgan Woods
Journal of Medicinal Chemistry | 1994
John W. Ellingboe; Madelene Antane; Nguyen Tt; Collini; Schuyler Adam Antane; Reinhold H. W. Bender; Hartupee D; White; McCallum J; Park Ch
Archive | 1995
Madelene Antane; John A. Butera; Bradford H. Hirth; Schuyler Adam Antane
Tetrahedron Letters | 2006
Zheng Wang; Hassan M. Elokdah; Geraldine Ruth Mcfarlane; Sherry Pan; Madelene Antane
Archive | 1998
Dominick Anthony Quagliato; Edward Martin Matelan; Madelene Antane
Journal of Medicinal Chemistry | 1998
John W. Ellingboe; Collini; Quagliato D; Chen J; Madelene Antane; Schmid J; Hartupee D; White; Park Ch; Tanikella T; Bagli Jf
Archive | 2002
Anthony F. Kreft; Madelene Antane; Derek Cecil Cole; Dennis M. Kubrak; Lynn Resnick; Joseph Raymond Stock; Zheng Wang