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

Autor:	Abedawn I. Khalaf, Colin J. Suckling, Andrew R. Pitt, Martin Scobie, Steven C. Young, Robert V. Fishleigh, Roger D. Waigh, William A. Wylie, John Urwin
Rok vydání:	2000
Předmět:	chemistry.chemical_classification Base pair Stereochemistry Organic Chemistry Biochemistry Footprinting Amino acid chemistry.chemical_compound Dicarboxylic acid chemistry Fluorenone Drug Discovery Phenanthrenes Selectivity DNA
Zdroj:	Tetrahedron. 56:5225-5239
ISSN:	0040-4020
DOI:	10.1016/s0040-4020(00)00432-4
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::7fb9e5f339a04c20c601575bc3e4a9ce https://doi.org/10.1016/s0040-4020(00)00432-4 Zobrazit plný text záznamu Full Text from ScienceDirect