Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372231 | Bioorganic & Medicinal Chemistry Letters | 2009 | 6 Pages |
Abstract
A serendipitous discovery that the metalloprotease binding profile of a novel class of 2-carboxamide-3-hydroxamic acid piperidines could be significantly attenuated by the modification of the unexplored P1 substituent enabled the design and synthesis of a novel 2-carboxamide-1-hydroxamic acid cyclohexyl scaffold core that exhibited excellent HER-2 potency and unprecedented MMP-selectivity that we believe would not have been possible via conventional P1′ perturbations.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
David M. Burns, Yun-Long Li, Eric Shi, Chunhong He, Meizhong Xu, Jincong Zhuo, Colin Zhang, Ding-Quan Qian, Yanlong Li, Richard Wynn, Maryanne B. Covington, Kamna Katiyar, Cindy A. Marando, Jordan S. Fridman, Peggy Scherle, Steve Friedman, Brian Metcalf,