2. Academic Validation
  3. Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents

Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents

  • Bioorg Med Chem Lett. 2007 Apr 15;17(8):2293-8. doi: 10.1016/j.bmcl.2007.01.056.
Cristina Martins 1,  Mekala Gunaratnam,  John Stuart,  Vaidahi Makwana,  Olga Greciano,  Anthony P Reszka,  Lloyd R Kelland,  Stephen Neidle
Affiliations

Affiliation

  • 1 CRUK Biomolecular Structure Group, The School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, United Kingdom.
PMID: 17276687 DOI: 10.1016/j.bmcl.2007.01.056
Abstract

The design, synthesis, biophysical and biochemical evaluation is presented of a new series of benzylamino-substituted acridines as G-quadruplex binding Telomerase inhibitors. Replacement of the previously reported anilino substituents by benzylamino groups results in enhanced quadruplex interaction, and for one compound, superior Telomerase inhibitory activity.

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