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

  • Kristopher E. Boyle
  • , Karen S. MacMillan
  • , David A. Ellis
  • , James P. Lajiness
  • , William M. Robertson
  • , Dale L. Boger

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Pages (from-to)1854-1857
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number6
DOIs
StatePublished - Mar 15 2010

ASJC Scopus Subject Areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Keywords

  • Antitumor drugs
  • DNA alkylating agents
  • Duocarmycins

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