Function through bio-inspired, synthesis-informed design: step-economical syntheses of designed kinase inhibitors
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- Function through bio-inspired, synthesis-informed design: step-economical syntheses of designed kinase inhibitors
- Wender, Paul A.; Axtman, Alison D.; Golden, Jennifer E.; Kee, Jung-Min; Sirois, Lauren E.; Quiroz, Ryan V.; Stevens, Matthew C.
- Issue Date
- Royal Society of Chemistry
- ORGANIC CHEMISTRY FRONTIERS, v.1, no.10, pp.1166 - 1171
- The human kinome comprises over 500 protein kinases. When mutated or over-expressed, many play critical roles in abnormal cellular functions associated with cancer, cardiovascular disease and neurological disorders. Here we report a step-economical approach to designed kinase inhibitors inspired by the potent, but non-selective, natural product staurosporine, and synthetically enabled by a novel, complexity-increasing, serialized [5 + 2]/[4 + 2] cycloaddition strategy. This function-oriented synthesis approach rapidly affords tunable scaffolds, and produced a low nanomolar inhibitor of protein kinase C.
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