D
Daniel L. Cheney
Researcher at Rhône-Poulenc
Publications - 13
Citations - 603
Daniel L. Cheney is an academic researcher from Rhône-Poulenc. The author has contributed to research in topics: Alkyl & Factor Xa Inhibitor. The author has an hindex of 9, co-authored 13 publications receiving 593 citations.
Papers
More filters
Journal ArticleDOI
New 4-point pharmacophore method for molecular similarity and diversity applications: overview of the method and applications, including a novel approach to the design of combinatorial libraries containing privileged substructures.
Jonathan S. Mason,Isabelle Morize,Menard Paul,Daniel L. Cheney,Christopher Hulme,Richard Labaudiniere +5 more
TL;DR: The details of the customized implementation of the method and its modification to systematically measure 4-point pharmacophores relative to a "special" substructure of interest present in the molecules under study are reported.
Journal ArticleDOI
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.
Ewing William R,Michael R. Becker,Vincent E. Manetta,Roderick S. Davis,Henry W. Pauls,Mason Helen J,Y.M. Choi-Sledeski,Daniel M. Green,Don D. Cha,Alfred P. Spada,Daniel L. Cheney,Jonathan S. Mason,Sebastien Maignan,Jean-Pierre Guilloteau,Karen D. Brown,Dennis J. Colussi,Ross Bentley,Jeff Bostwick,Charles Kasiewski,Suzanne Morgan,Robert J. Leadley,Christopher T. Dunwiddie,Mark H. Perrone,Valeria Chu +23 more
TL;DR: RPR120844, a potent inhibitor of FXa which shows selectivity for FXa over trypsin, thrombin, and several fibrinolytic serine proteinases, is an effective anticoagulant in both the rat model of FeCl(2)-induced carotid artery thrombosis and the rabbit model of jugular vein thrombus formation.
Journal ArticleDOI
The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4-d]pyrimidines, inhibitors of CSF-1R tyrosine kinase activity
Myers Michael R,Natalie N. Setzer,Alfred P. Spada,Persons Paul E,Cuong Ly,Martin P. Maguire,Allison L. Zulli,Daniel L. Cheney,Asher Zilberstein,Susan E. Johnson,Carol Franks,Karen J. Mitchell +11 more
TL;DR: In this paper, moderately potent and selective inhibitors of CSF-1R tyrosine kinase activity were identified, and a preliminary SAR study resulted in the identification of compounds 11 and 20 as the most potent analogues in the series (IC50 = 0.18 μM) and showed that the 3-D-conformation of 4-(N-alkyl-N-phenyl)-aminoquinazolines has been important to the overall selectivity and activity.
Journal ArticleDOI
Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization.
Y.M. Choi-Sledeski,Mcgarry Daniel G,Daniel M. Green,Helen J. Mason,Michael R. Becker,Davis Roderick S,William R. Ewing,William P. Dankulich,Vincent E. Manetta,Robert L. Morris,Spada Alfred P,Daniel L. Cheney,Karen Brown,Dennis Colussi,Valeria Chu,Christopher L. Heran,Suzanne R Morgan,Ross G. Bentley,Robert J. Leadley,Sébastien Maignan,Jean-Pierre Guilloteau,Dunwiddie Christopher T,Pauls Henry W +22 more
TL;DR: X-ray crystallographic experiments in trypsin and molecular modeling studies suggest that the sulfonamidopyrrolidinones inhibitors bind by insertion of the 4-hydroxybenzamidine moiety into the S-1 subsite of the fXa active site.
Proceedings ArticleDOI
Library design and virtual screening using multiple 4-point pharmacophore fingerprints.
TL;DR: A new extension to the method for structure-based design is reported that uses the shape of the target site as an additional constraint, which enables the docking process to be quantified in terms of how many, and which, pharmacophoric hypotheses can be matched by a compound or a library of compounds.