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Hit-to-lead optimization and kinase selectivity of imidazo[1,2-a]quinoxalin-4-amine derived JNK1 inhibitors. 2013
Bei Li, and
Oana M Cociorva, and
Tyzoon Nomanbhoy, and
Helge Weissig, and
Qiang Li, and
Kai Nakamura, and
Marek Liyanage, and
Melissa C Zhang, and
Ann Y Shih, and
Arwin Aban, and
Yi Hu, and
Julia Cajica, and
Lan Pham, and
John W Kozarich, and
Kevin R Shreder
ActivX Biosciences, Inc., 11025 N. Torrey Pines Road, La Jolla, CA 92037, USA.
As the result of a rhJNK1 HTS, the imidazo[1,2-a]quinoxaline 1 was identified as a 1.6 μM rhJNK1 inhibitor. Optimization of this compound lead to AX13587 (rhJNK1 IC50=160 nM) which was co-crystallized with JNK1 to identify key molecular interactions. Kinase profiling against 125+ kinases revealed AX13587 was an inhibitor of JNK, MAST3, and MAST4 whereas its methylene homolog AX14373 (native JNK1 IC50=47 nM) was a highly specific JNK inhibitor.
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