Leslie Leith
Bristol-Myers Squibb
14 Papers
151 Citations
Leslie Leith is an academic researcher from Bristol-Myers Squibb. The author has contributed to research in topics: Chemistry & Hydantoin. The author has an hindex of 10, co-authored 13 publications.
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Papers
Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects.
Kyoung S. Kim,John S. Sack,John S. Tokarski,Ligang Qian,Sam T. Chao,Leslie Leith,Y. F. Kelly,Raj N. Misra,John T. Hunt,Kimball Sd,William G. Humphreys,Barri Wautlet,Janet G. Mulheron,K R Webster +13 more
TL;DR: CDK1 selective thio- and oxoflavopiridol analogues inhibit the colony-forming ability of multiple human tumor cell lines and possess a unique antiproliferative profile in comparison to flavopirodol.
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Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.
Natesan Murugesan,Zhengxiang Gu,Steven H. Spergel,Marian Young,Ping Chen,Arvind Mathur,Leslie Leith,Mark A. Hermsmeier,Eddie C.-K. Liu,Rongan Zhang,Eileen Bird,T.L. Waldron,Anthony M. Marino,Barry Koplowitz,W. Griffith Humphreys,Saeho Chong,Richard A. Morrison,Maria L. Webb,Suzanne Moreland,Nick C. Trippodo,Joel C. Barrish +20 more
TL;DR: The 3-amino-isoxazole group was combined with the optimal 2'-substituent leading to 16a, an extremely potent and selective ET(A) receptor antagonist that was 100% in rats and the systemic clearance and volume of distribution are higher than that of 1.
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Discovery and Development of 5-[(5S,9R)-9- (4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1- methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non- 7-yl-methyl]-3-thiophenecarboxylic Acid (BMS-587101)A Small Molecule Antagonist of Leukocyte Function Associated Antigen-1†
Dominique Potin,Michele Launay,Francoise Monatlik,Patrice Malabre,Maud Fabreguettes,Andre Fouquet,Magali Maillet,Eric Nicolai,Loïc Dorgeret,François Chevallier,Dominique Besse,Monique Dufort,Francois Caussade,Syed Zamberi Ahmad,Dawn K. Stetsko,Stacey Skala,Patricia M. Davis,Praveen Balimane,Karishma Patel,Zheng Yang,Punit Marathe,Jennifer Postelneck,Robert M. Townsend,Valentina Goldfarb,Steven Sheriff,Howard Einspahr,Kevin Kish,Mary F. Malley,John D. Dimarco,Jack Z. Gougoutas,Pathanjali Kadiyala,Daniel L. Cheney,Ravindra W. Tejwani,Murphy Denette K,Kim W. McIntyre,Xiaoxia Yang,Sam T. Chao,Leslie Leith,Zili Xiao,Arvind Mathur,Bang-Chi Chen,Daugh-Rurng Wu,Sarah C. Traeger,Murray McKinnon,Joel C. Barrish,Jeffrey A. Robl,Edwin J. Iwanowicz,Suzanne J. Suchard,T. G. Murali Dhar +48 more
TL;DR: The discovery and preliminary SAR of spirocyclic hydantoin based LFA-1 antagonists that culminated in the identification of analog 8 as a clinical candidate are described and the first example of the efficacy of a small molecule L FA-1 antagonist in combination with CTLA-4Ig in an animal model of transplant rejection is reported.
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The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.
Aaron Balog,Mark E. Salvati,Weifang Shan,Arvind Mathur,Leslie Leith,Donna D. Wei,Ricardo M. Attar,Jieping Geng,Cheryl A. Rizzo,Chihuei Wang,Stanley R. Krystek,John S. Tokarski,John T. Hunt,Marco M. Gottardis,Roberto Weinmann +14 more
TL;DR: A novel series of [2.2.1]-azahydantoins has been designed and synthesized in an enantiospecific manner and several were found to have potent activity in vitro.
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Biphenylsulfonamide Endothelin Receptor Antagonists. 2. Discovery of 4‘-Oxazolyl Biphenylsulfonamides as a New Class of Potent, Highly Selective ETA Antagonists
Natesan Murugesan,Zhengxiang Gu,Philip D. Stein,Steven H. Spergel,Arvind Mathur,Leslie Leith,Eddie C.-K. Liu,Rongan Zhang,Eileen Bird,T.L. Waldron,Anthony M. Marino,Richard A. Morrison,Maria L. Webb,Suzanne Moreland,Joel C. Barrish +14 more
TL;DR: The synthesis and structure-activity relationship (SAR) studies of a series of 4'-oxazolyl-N-(3,4-dimethyl-5-isoxzolyl)[1, 1'-biphenyl]-2-sulfonamide derivatives as endothelin-A (ET(A)) receptor antagonists reveal a remarkable improvement in potency and metabolic stability when the 4'-position of the biphenylsulf onamide is substituted with an oxazole
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