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Substituent effects within the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065

Academic Article
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Overview

authors

  • Boger, Dale
  • Stauffer, F.
  • Hedrick, M. P.

publication date

  • August 2001

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

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.

subject areas

  • Adenine
  • Alkylation
  • Antibiotics, Antineoplastic
  • Binding Sites
  • DNA
  • DNA Adducts
  • Humans
  • Indoles
  • Inhibitory Concentration 50
  • Leucomycins
  • Nucleic Acid Conformation
  • Pyrroles
  • Pyrrolidinones
  • Tumor Cells, Cultured
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/s0960-894x(01)00372-9

PubMed ID

  • 11454471
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Additional Document Info

start page

  • 2021

end page

  • 2024

volume

  • 11

issue

  • 15

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