Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376497 | Bioorganic & Medicinal Chemistry Letters | 2006 | 6 Pages |
Abstract
The development of potent, orally bioavailable, and selective series of 5-amino-3-hydroxy-N(1-hydroxypropane-2-yl)isothiazole-4-carboxamidine inhibitors of MEK1 and MEK-2 kinase is described. Optimization of the carboxamidine and the phenoxyaniline group led to the identification of 55 which gave good potency as in vitro MEK1 inhibitors, and good oral exposure in rat.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Hassan El Abdellaoui, Chamakura V.N.S. Varaprasad, Dinesh Barawkar, Subrata Chakravarty, Andreas Maderna, Robert Tam, Huanming Chen, Matt Allan, Jim Z. Wu, Todd Appleby, Shunqi Yan, Weijian Zhang, Stanley Lang, Nanhua Yao, Robert Hamatake, Zhi Hong,