Synthesis and evaluation of a thio analogue of duocarmycin SA |
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Authors: | Karen S MacMillan James P Lajiness Carlota Lopez Cara Romeo Romagnoli William M Robertson Inkyu Hwang Pier Giovanni Baraldi Dale L Boger |
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Institution: | 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;2. Dipartimento di Scienze Farmaceutiche,Università degli Studi di Ferrara, Via Fossato di Mortara 17/19, 44100 Ferrara, Italy |
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Abstract: | The design, synthesis, and preliminary evaluation of methyl 1,2,8,8a-tetrahydrocyclopropac]thieno3,2-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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