Structure-driven HtL: Design and synthesis of novel aminoindazole inhibitors of c-Jun N-terminal kinase activity

The design and synthesis of a new series of c-Jun N-terminal kinase inhibitors are reported. The novel series of substituted amino indazoles were designed based on a combination of hits from high-throughput screening and X-ray crystal structure information of the compounds crystallised into the JNK-1 ATP binding site.

Graphical abstractThe design and synthesis of a new series of c-Jun N-terminal kinase inhibitors are reported. Compound 23 displayed the greatest activity within the series.Figure optionsDownload full-size imageDownload as PowerPoint slide