ArticleOrganic chemistry frontiers : an international journal of organic chemistry2014
Function through bio-inspired, synthesis-informed design: step-economical syntheses of designed kinase inhibitors†Dedicated to Max Malacria, a friend and scholar whose science and creative contributions to step-economical synthesis have inspired us all and moved the field closer to the ideal.‡Electronic supplementary information (ESI) available: Synthetic procedures and spectral data. See DOI: 10.1039/c4qo00228hClick here for additional data file.
Article in Organic chemistry frontiers : an international journal of organic chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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4 citing papers in PubMed, 6 citations in OpenAlex.
- Staurosporine as an Antifungal Agent.International journal of molecular sciences · 2025Review
- Staurosporine: new lease of life for parent compound of today's novel and highly successful anti-cancer drugs.The Journal of antibiotics · 2018Review
- Ynol Ethers as Ketene Equivalents in Rhodium-Catalyzed Intermolecular [5 + 2] Cycloaddition Reactions.Organic letters · 2017Article
- Function through synthesis-informed design.Accounts of chemical research · 2015Article
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
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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Registered trials
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