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Establishment of substituent effects in the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065

Academic Article
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Overview

related to degree

  • Kastrinsky, David, Ph.D. in Synthetic Organic Chemistry, Scripps Research 2000 - 2005

authors

  • Parrish, J. P.
  • Kastrinsky, David
  • Stauffer, F.
  • Hedrick, M. P.
  • Hwang, I.
  • Boger, Dale

publication date

  • August 2003

journal

  • Bioorganic & Medicinal Chemistry  Journal

abstract

  • An extensive series of CBI analogues of the duocarmycins and CC-1065 exploring substituent effects within the first indole DNA binding subunit is detailed. In general, substitution at the indole C5 position led to cytotoxic potency enhancements that can be >/=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

  • Alkylation
  • Amides
  • DNA
  • Indoles
  • Kinetics
  • Models, Molecular
  • Pyrroles
  • Pyrrolidinones
  • Sulfones
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Identity

International Standard Serial Number (ISSN)

  • 0968-0896

Digital Object Identifier (DOI)

  • 10.1016/s0968-0896(03)00194-9

PubMed ID

  • 12901927
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Additional Document Info

start page

  • 3815

end page

  • 3838

volume

  • 11

issue

  • 17

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