| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1358696 | Bioorganic & Medicinal Chemistry Letters | 2015 | 5 Pages |
Abstract
A series of structure based drug design hypotheses and focused screening efforts led to the identification of tetrahydropyrrolo-diazepenones with striking potency against ERK2 kinase. The role of fluorination in mitigating microsomal clearance was systematically explored. Ultimately, it was found that fluorination of a cyclopentanol substructure provided significant improvement in both potency and human metabolic stability.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jeffrey T. Bagdanoff, Rama Jain, Wooseok Han, Shejin Zhu, Ann-Marie Madiera, Patrick S. Lee, Xiaolei Ma, Daniel Poon,