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Your search keyword '"Michael E. Prime"' showing total 2 results
Start Over Author "Michael E. Prime" Journal journal of medicinal chemistry
2 results on '"Michael E. Prime"'

1. Design and Evaluation of [18F]CHDI-650 as a Positron Emission Tomography Ligand to Image Mutant Huntingtin Aggregates

Author

Longbin Liu, Peter D. Johnson, Michael E. Prime, Vinod Khetarpal, Christopher J. Brown, Luca Anzillotti, Daniele Bertoglio, Xuemei Chen, Samuel Coe, Randall Davis, Anthony P. Dickie, Simone Esposito, Elise Gadouleau, Paul R. Giles, Catherine Greenaway, James Haber, Christer Halldin, Scott Haller, Sarah Hayes, Todd Herbst, Frank Herrmann, Manuela Heßmann, Ming Min Hsai, Yaser Khani, Adrian Kotey, Angelo Lembo, John E. Mangette, Gwendolyn A. Marriner, Richard W. Marston, Matthew R. Mills, Edith Monteagudo, Anton Forsberg-Morén, Sangram Nag, Laura Orsatti, Christine Sandiego, Sabine Schaertl, Joanne Sproston, Steven Staelens, Jack Tookey, Penelope A. Turner, Andrea Vecchi, Maria Veneziano, Ignacio Muñoz-Sanjuan, Jonathan Bard, and Celia Dominguez

Subjects
Drug Discovery, Molecular Medicine, Settore CHIM/08 - Chimica Farmaceutica, Settore CHIM/06
Published
2022

2. Phthalazinone Pyrazoles as Potent, Selective, and Orally Bioavailable Inhibitors of Aurora-A Kinase.

Author

Michael E. Prime, Stephen M. Courtney, Frederick A. Brookfield, Richard W. Marston, Victoria Walker, Justin Warne, Andrew E. Boyd, Norman A. Kairies, Wolfgang von der Saal, Anja Limberg, Guy Georges, Richard A. Engh, Bernhard Goller, Petra Rueger, and Matthias Rueth

Subjects
*PYRAZOLES, *DRUG synergism, *DRUG bioavailability, *AURORAS, *PROTEIN kinases, *MITOSIS, *TUMOR growth, *APOPTOSIS, *CANCER cell proliferation
Abstract

The inhibition of Aurora kinases in order to arrest mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells has generated significant discussion within the literature. We report a novel class of Aurora kinase inhibitors based upon a phthalazinone pyrazole scaffold. The development of the phthalazinone template resulted in a potent Aurora-A selective series of compounds (typically >1000-fold selectivity over Aurora-B) that display good pharmacological profiles with significantly improved oral bioavailability compared to the well studied Aurora inhibitor VX-680. [ABSTRACT FROM AUTHOR]

Published
2011
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