| Literature DB >> 16934458 |
Hassan El Abdellaoui1, 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.
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.Entities:
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Year: 2006 PMID： 16934458 DOI： 10.1016/j.bmcl.2006.08.048
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823