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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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.
| Author(s): | Khalaf, A.I., Pitt, A.R., Scobie, M., Suckling, C.J., Urwin, J., Waigh, R.D., Young, S.C., Fishleigh, R.V. and Wylie, W.A. | Item type: | Article |
|---|---|
| ID code: | 715 |
| Keywords: | DNA, minor groove, lexitropsin dimer, synthesis, Chemistry |
| Subjects: | Science > Chemistry |
| Department: | Faculty of Science > Pure and Applied Chemistry Unknown Department Faculty of Science > Strathclyde Institute of Pharmacy and Biomedical Sciences |
| Depositing user: | Allison Crawford |
| Date deposited: | 05 Apr 2006 |
| Last modified: | 03 May 2019 02:01 |
| URI: | https://strathprints.strath.ac.uk/id/eprint/715 |
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