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  • Title: Substituent effects within the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065.
    Author: Boger DL, Stauffer F, Hedrick MP.
    Journal: Bioorg Med Chem Lett; 2001 Aug 06; 11(15):2021-4. PubMed ID: 11454471.
    Abstract:
    A series of CBI analogues of the duocarmycins and CC-1065 exploring substituent effects within the first indole DNA binding subunit are detailed. Substitution at the indole C5 position led to cytotoxic potency enhancements that are > or =1000-fold, providing simplified analogues containing a single DNA binding subunit that are more potent (IC(50)=2-3 pM) than CBI-TMI, duocarmycin SA, or CC-1065.
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