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Your search keyword '"Julia M. Ford Pulido"' showing total 2 results
Start Over Author "Julia M. Ford Pulido" Topic biochemistry
2 results on '"Julia M. Ford Pulido"'

1. Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors

Author

Michael J. Hadd, Helen Hua, Gang Liu, Dana Gitnick, Troy D. Vickers, Lan Tran, Janice A. Sindac, Joyce James, Zdravko V. Milanov, Robert C. Armstrong, Daniel K. Treiber, Mark W. Holladay, Julia M. Ford Pulido, Merryl D. Cramer, Barbara Belli, Shripad Bhagwat, Alan Dao, and Sunny Abraham

Subjects
medicine.drug_class, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Carboxamide, Protein Serine-Threonine Kinases, Mitogen-activated protein kinase kinase, Biochemistry, MAP2K7, Structure-Activity Relationship, Aurora kinase, Aurora Kinases, Drug Discovery, medicine, Protein Kinase Inhibitors, Molecular Biology, Serine/threonine-specific protein kinase, Dose-Response Relationship, Drug, Molecular Structure, biology, Triazines, Chemistry, Cyclin-dependent kinase 4, Kinase, Organic Chemistry, Cyclin-dependent kinase 2, Stereoisomerism, biology.protein, Molecular Medicine
Abstract

The synthesis and SAR for a novel series of pyrrolotriazines as pan-Aurora kinase inhibitors are described. Optimization of the cyclopropane carboxamide terminus of lead compound 1 resulted in analogs with high cellular activity and improved rat PK profiles. Notably, compound 17l demonstrated tumor growth inhibition in a mouse xenograft model.

Published
2011
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2. Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases

Author

Dana Gitnick, Gang Liu, Julia M. Ford Pulido, Mike A. Breider, Daniel K. Treiber, Joyce K. James, Robert C. Armstrong, Michael F. Gardner, Brian T. Campbell, Barbara A. Belli, Daniel Brigham, Mark W. Holladay, and Helen Hua

Subjects
biology, Kinase, business.industry, Growth factor, medicine.medical_treatment, Inflammatory arthritis, Organic Chemistry, Arthritis, Pharmacology, medicine.disease, Biochemistry, Pharmacokinetics, In vivo, Tolerability Study, Drug Discovery, biology.protein, medicine, business, Platelet-derived growth factor receptor
Abstract

A series of potent, selective platelet-derived growth factor receptor-family kinase inhibitors was optimized starting from a globally selective lead molecule 4 through structural modifications aimed at improving the physiochemical and pharmacokinetic properties, as exemplified by 18b. Further clearance reduction via per-methylation of the α-carbons of a solubilizing piperidine nitrogen resulted in advanced leads 22a and 22b. Results from a mouse tumor xenograft, a collagen-induced arthritis model, and a 7 day rat in vivo tolerability study culminated in the selection of compound 22b (AC710) as a preclinical development candidate.

Published
2012

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