Marcel Koenig

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Organization: The Scripps Research Institute

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Chemicals
References

Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors

Co-reporter:Yuanjun He, Derek Duckett, Weimin Chen, Yuan Yuan Ling, Michael D. Cameron, Li Lin, Claudia H. Ruiz, Philip V. LoGrasso, Theodore M. Kamenecka, Marcel Koenig

Bioorganic & Medicinal Chemistry Letters 2014 Volume 24(Issue 1) pp:161-164

Publication Date(Web):1 January 2014

DOI:10.1016/j.bmcl.2013.11.052

Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) Inhibitors

Co-reporter:Yuanjun He, Theodore M. Kamenecka, Youseung Shin, Xinyi Song, Rong Jiang, Romain Noel, Derek Duckett, Weimin Chen, Yuan Yuan Ling, Michael D. Cameron, Li Lin, Susan Khan, Marcel Koenig, Philip V. LoGrasso

Bioorganic & Medicinal Chemistry Letters 2011 Volume 21(Issue 6) pp:1719-1723

Publication Date(Web):15 March 2011

DOI:10.1016/j.bmcl.2011.01.079

Quinazoline 3 was discovered as a novel c-jun N-terminal kinase (JNK) inhibitor with good brain penetration and pharmacokinetic (PK) properties. A number of analogs which were potent both in the biochemical and cellular assays were discovered. Quinazoline 13a was found to be a potent JNK3 inhibitor (IC50 = 40 nM), with >500-fold selectivity over p38, and had good PK and brain penetration properties. With these properties, 13a is considered a potential candidate for in vivo evaluation.Quinazolines 3 and 13a were discovered as novel c-jun N-terminal kinase (JNK) inhibitors with good brain penetration and pharmacokinetic (PK) properties. Compound 13a is considered a potential candidate for in vivo evaluation.