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기정민

Kee, Jung-Min
Bioorganic and Chembio Lab.
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Function through bio-inspired, synthesis-informed design: step-economical syntheses of designed kinase inhibitors

Author(s)
Wender, Paul A.Axtman, Alison D.Golden, Jennifer E.Kee, Jung-MinSirois, Lauren E.Quiroz, Ryan V.Stevens, Matthew C.
Issued Date
2014-12
DOI
10.1039/c4qo00228h
URI
https://scholarworks.unist.ac.kr/handle/201301/10810
Fulltext
http://pubs.rsc.org/en/Content/ArticleLanding/2014/QO/C4QO00228H#!divAbstract
Citation
ORGANIC CHEMISTRY FRONTIERS, v.1, no.10, pp.1166 - 1171
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.
Publisher
Royal Society of Chemistry
ISSN
2052-4129

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