The Synthesis of Some Head to Head Linked DNA Minor Groove Binders

A.I. Khalaf, A.R. Pitt, M. Scobie, C.J. Suckling, J. Urwin, R.D. Waigh, S.C. Young, R.V. Fishleigh, W.A. Wylie

Research output: Contribution to journalArticlepeer-review

36 Citations (Scopus)


A series of head to head linked dimers of heterocyclic amino acids has been prepared for investigation of affinity and selectivity in binding to the minor groove of DNA. The selection of targets for synthesis was led by computer based design. Several novel dicarboxylic acid linkers including indoles, phenanthrenes, a fluorenone, and a bisbenzothiophene have been included. Analysis of binding to DNA by footprinting showed high affinity for compounds derived from 2,7-dihydrophenanthrene dicarboxylic acid and a predominant selectivity for AT rich regions containing at least 4 AT pairs but with the ability to span up to two CG base pairs.
Original languageEnglish
Pages (from-to)5225-5239
Number of pages14
JournalInternational Journal of Chemical Research
Issue number29
Publication statusPublished - 14 Jul 2000


  • DNA
  • minor groove
  • lexitropsin dimer
  • synthesis


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