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The Strathprints institutional repository is a digital archive of University of Strathclyde research outputs.

Strathprints serves world leading Open Access research by the University of Strathclyde, including research by the Strathclyde Institute of Pharmacy and Biomedical Sciences (SIPBS), where research centres such as the Industrial Biotechnology Innovation Centre (IBioIC), the Cancer Research UK Formulation Unit, SeaBioTech and the Centre for Biophotonics are based.

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

Khalaf, A.I. and Pitt, A.R. and Scobie, M. and Suckling, C.J. and Urwin, J. and Waigh, R.D. and Young, S.C. and Fishleigh, R.V. and Wylie, W.A. (2000) The Synthesis of Some Head to Head Linked DNA Minor Groove Binders. International Journal of Chemical Research, 56 (29). pp. 5225-5239. ISSN 0975-3699

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Abstract

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.