Tetrahedron

The synthesis of some head to head linked DNA minor groove binders

AI Khalaf, AR Pitt, M Scobie, CJ Suckling, J Urwin…

文献索引：Khalaf, Abedawn I.; Pitt, Andrew R.; Scobie, Martin; Suckling, Colin J.; Urwin, John; Waigh, Roger D.; Fishleigh, Robert V.; Young, Steven C.; Wylie, William A. Tetrahedron, 2000 , vol. 56, # 29 p. 5225 - 5239

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被引用次数: 34

摘要

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 ...