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  • Title: A novel approach to the synthesis of cytotoxic C2-C3 unsaturated pyrrolo[2,1-c]benzodiazepines (PBDs) with conjugated acrylyl C2-substituents.
    Author: Chen Z, Gregson SJ, Howard PW, Thurston DE.
    Journal: Bioorg Med Chem Lett; 2004 Mar 22; 14(6):1547-9. PubMed ID: 15006400.
    Abstract:
    A concise synthesis of three novel C2-C3 unsaturated pyrrolo[2,1-c][1,4]benzodiazepine analogues (18-20) containing conjugated acrylyl C2-substituents is reported that utilises Heck coupling to install the C2-acrylyl side chains. These analogues possess significant cytotoxicity according to the NCI 60-cell line screen with 18 surpassing anthramycin (1) in potency.
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