C
Cynthia A. Parrish
Researcher at GlaxoSmithKline
Publications - 30
Citations - 1160
Cynthia A. Parrish is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Fatty acid synthase & Cancer. The author has an hindex of 14, co-authored 30 publications receiving 1068 citations.
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Journal ArticleDOI
Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin
Steven D. Knight,Nicholas D. Adams,Joelle Lorraine Burgess,Amita M. Chaudhari,Michael G. Darcy,Carla A. Donatelli,Juan I. Luengo,Ken A. Newlander,Cynthia A. Parrish,Lance Ridgers,Martha A. Sarpong,Schmidt Stanley J,Glenn S. Van Aller,Jeffrey D. Carson,Melody Diamond,Patricia A. Elkins,Christine M. Gardiner,Eric Garver,Seth A. Gilbert,Richard R. Gontarek,Jeffrey R. Jackson,Kevin L. Kershner,Lusong Luo,Kaushik Raha,Christian S. Sherk,Chiu-Mei Sung,David Sutton,Peter J. Tummino,Ronald Wegrzyn,Kurt R. Auger,Dashyant Dhanak +30 more
TL;DR: 2,4-Difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3- pyridinyl}benzenesulfonamide (GSK2126458, 1) has been identified as a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.
Journal ArticleDOI
ATP-competitive inhibitors of the mitotic kinesin KSP that function via an allosteric mechanism.
Lusong Luo,Cynthia A. Parrish,Neysa Nevins,Dean E. McNulty,Amita M. Chaudhari,Jeffery D Carson,Valery Sudakin,Antony N. Shaw,Ruth Lehr,Huizhen Zhao,Sharon Sweitzer,Latesh Lad,Kenneth W. Wood,Roman Sakowicz,Roland S. Annan,Pearl S. Huang,Pearl S. Huang,Jeffrey R. Jackson,Dashyant Dhanak,Robert A. Copeland,Kurt R. Auger +20 more
TL;DR: A new class of selective KSP inhibitors that are active against ispinesib-resistant forms of KSP are described, suggesting that they compete with ATP binding via a novel allosteric mechanism.
Journal ArticleDOI
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase
Nicholas D. Adams,Jerry L. Adams,Joelle Lorraine Burgess,Amita M. Chaudhari,Robert A. Copeland,Carla A. Donatelli,David H. Drewry,Kelly E. Fisher,Toshihiro Hamajima,Mary Ann Hardwicke,William F. Huffman,Kristin K Koretke-Brown,Zhihong V Lai,Octerloney B. McDonald,Hiroko Nakamura,Ken A. Newlander,Catherine A. Oleykowski,Cynthia A. Parrish,Denis R. Patrick,Ramona Plant,Martha A. Sarpong,Kosuke Sasaki,Schmidt Stanley J,Domingos J. Silva,David Sutton,Jun Tang,Christine Thompson,Peter J. Tummino,Jamin C Wang,Hong Xiang,Jingsong Yang,Dashyant Dhanak +31 more
TL;DR: Key to the advancement of the series was the introduction of a 2-aryl group containing a basic amine onto the azaindole leading to significantly improved cellular activity leading to the identification of GSK1070916 (17k), a potent and selective ATP-competitive inhibitor of Aurora B and C.
Journal ArticleDOI
Novel ATP-competitive kinesin spindle protein inhibitors.
Cynthia A. Parrish,Nicholas D. Adams,Kurt R. Auger,Joelle Lorraine Burgess,Jeffrey D. Carson,Amita M. Chaudhari,Robert A. Copeland,Melody Diamond,Carla A. Donatelli,Kevin J. Duffy,Leo F. Faucette,Jeffrey T. Finer,William F. Huffman,Erin D. Hugger,Jeffrey R. Jackson,Steven D. Knight,Lusong Luo,Michael L. Moore,Ken A. Newlander,Lance Ridgers,Roman Sakowicz,Antony N. Shaw,Chiu-Mei M Sung,David Sutton,Kenneth W. Wood,Shu-Yun Zhang,Michael N. Zimmerman,Dashyant Dhanak +27 more
TL;DR: In a murine xenograft model with HCT116 D130V tumors, 20 showed significant antitumor activity following intraperitoneal dosing, providing in vivo proof-of-principle of the efficacy of an ATP-competitive KSP inhibitor versus tumors that are resistant to the other known KSP inhibitors.
Patent
Azaindole inhibitors of aurora kinases
Jerry L. Adams,Nicholas D. Adams,Jeffrey M. Axten,Amita M. Chaudhari,Dashyant Dhanak,Toshihiro Hamajima,Kenneth A. Newlander,Cynthia A. Parrish,Martha A. Sarpong,Silva Domingos J,Jun Tang +10 more
TL;DR: The present invention relates to a compound represented by Formula (I): and pharmaceutically acceptable salts, making them especially suitable for the treatment of a number of diseases, including solid tumor cancers and hematological cancers.