期刊
Organic Chemistry Frontiers
卷 1, 期 10, 页码 1166-1171出版社
CHINESE CHEMICAL SOC
DOI: 10.1039/c4qo00228h
关键词
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资金
- NIH [ROI CA031845]
- NSF Graduate Research Fellowships
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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