Rapid synthesis and zebrafish evaluation of a phenanthridine-based small molecule library |
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Authors: | Donaldson Lauren R Wallace Stephen Haigh David Patton E Elizabeth Hulme Alison N |
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Institution: | School of Chemistry, The University of Edinburgh, West Mains Road, Edinburgh, UK EH9 3JJ. |
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Abstract: | A Heck cyclisation approach is described for the rapid synthesis of a library of natural product-like small molecules, based on the phenanthridine core. The synthesis of a range of substituted benzylamine building blocks and their incorporation into the library is reported, together with a highly selective cis-dihydroxylation protocol that enables access to the target compounds in an efficient manner. Biological evaluation of the library using zebrafish phenotyping has led to the discovery of compound 20c, a novel inhibitor of early-stage zebrafish embryo development. |
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