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Design, synthesis and evaluation of bouvardin, deoxybouvardin and RA-I-XIV pharmacophore analogs

Academic Article
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Overview

authors

  • Boger, Dale
  • Patane, M. A.
  • Jin, Q.
  • Kitos, P. A.

publication date

  • 1994

journal

  • Bioorganic & Medicinal Chemistry  Journal

abstract

  • The synthesis and in vitro cytotoxic evaluation of a key set of cycloisodityrosine subunit analogs of deoxybouvardin and RA-VII are detailed and constitute a complete investigation of the natural product pharmacophore. The studies illustrate that the 18-membered ring tetrapeptide potentiation of the cytotoxic activity of cycloisodityrosine is not likely to be due to simple alteration or constraint of the conformation of the 14-membered cycloisodityrosine subunit and that simple derivatization of cycloisodityrosine may not provide the same potentiation.

subject areas

  • Animals
  • Antibiotics, Antineoplastic
  • Antineoplastic Agents, Phytogenic
  • Drug Design
  • Drug Screening Assays, Antitumor
  • In Vitro Techniques
  • Leukemia L1210
  • Magnetic Resonance Spectroscopy
  • Mice
  • Molecular Structure
  • Peptides, Cyclic
  • Protein Conformation
  • Structure-Activity Relationship
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Identity

International Standard Serial Number (ISSN)

  • 0968-0896

Digital Object Identifier (DOI)

  • 10.1016/s0968-0896(00)82005-2

PubMed ID

  • 7922127
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Additional Document Info

start page

  • 85

end page

  • 100

volume

  • 2

issue

  • Copyright (C) 2014 American Chemical Society (ACS). All Rights Reserved.

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