Synthesis and evaluation of a thio analogue of duocarmycin SA

  • Bioorg Med Chem Lett. 2009 Dec 15;19(24):6962-5. doi: 10.1016/j.bmcl.2009.10.063.
Karen S MacMillan  1 ,  James P Lajiness ,  Carlota Lopez Cara ,  Romeo Romagnoli ,  William M Robertson ,  Inkyu Hwang ,  Pier Giovanni Baraldi ,  Dale L Boger
Affiliations
  • 1. Department of Chemistry and the Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
PMID: 19879753 DOI: 10.1016/j.bmcl.2009.10.063
Abstract

The design, synthesis, and preliminary evaluation of methyl 1,2,8,8a-tetrahydrocyclopropa[c]thieno[3,2-e]indol-4-one-6-carboxylate (CTI) derivatives are detailed representing a single atom change (N to S) embedded in the duocarmycin SA alkylation subunit.

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