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Establishing the parabolic relationship between reactivity and activity for derivatives and analogues of the duocarmycin and CC-1065 alkylation subunits

Academic Article
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Overview

authors

  • Parrish, J. P.
  • Hughes, T. V.
  • Hwang, I. Y.
  • Boger, Dale

publication date

  • January 2004

journal

  • Journal of the American Chemical Society  Journal

abstract

  • The preparation of a novel series of N-aryl CBI derivatives is detailed in which an aryl para substituent could be used to predictably modulate the reactivity of the resulting CC-1065/duocarmycin alkylation subunit analogue (rho = 0.17). The derivatives were found to be exceptionally stable and to exhibit a well-defined relationship between reactivity and cytotoxic potency. When combined with the results of an extensive series of N-acyl CBI analogues and derivatives assembled over the past 15 years, the studies define a fundamental parabolic relationship between reactivity and cytotoxic potency.

subject areas

  • Alkylation
  • Animals
  • Antibiotics, Antineoplastic
  • Drug Screening Assays, Antitumor
  • Indoles
  • Leukemia L1210
  • Mice
  • Pyrrolidinones
  • Structure-Activity Relationship
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Identity

International Standard Serial Number (ISSN)

  • 0002-7863

Digital Object Identifier (DOI)

  • 10.1021/ja038162t

PubMed ID

  • 14709069
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Additional Document Info

start page

  • 80

end page

  • 81

volume

  • 126

issue

  • 1

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