Rapid synthesis and zebrafish evaluation of a phenanthridine-based small molecule library

L.R. Donaldson, S. Wallace, David Haigh, E.E. Patton, A.N. Hulme

Research output: Contribution to journalArticle

13 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)2233-2239
Number of pages7
JournalOrganic and Biomolecular Chemistry
Volume9
Issue number7
DOIs
Publication statusPublished - 07 Apr 2011

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Biochemistry

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