Synthesis and evaluation of duocarmycin SA analogs incorporating the methyl 1,2,8,8a-tetrahydrocyclopropa[c]oxazolo[2,3-e]indol-4-one-6-carboxylate (COI) alkylation subunit

  • Bioorg Med Chem Lett. 2010 Mar 15;20(6):1854-7. doi: 10.1016/j.bmcl.2010.01.145.
Kristopher E Boyle  1 ,  Karen S MacMillan ,  David A Ellis ,  James P Lajiness ,  William M Robertson ,  Dale L Boger
Affiliations
  • 1. Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
PMID: 20171886 DOI: 10.1016/j.bmcl.2010.01.145
Abstract

The design, synthesis and evaluation of methyl 1,2,8,8a-tetrahydrocyclopropa[c]oxazolo[2,3-e]indol-4-one-6-carboxylate (COI) derivatives are detailed representing analogs of duocarmycin SA containing an oxazole replacement for the fused pyrrole found in the alkylation subunit.