Amplification of DNA-binding affinities of protoberberine alkaloids by appended polyamines.

Basic Information

ID: ALA1146310

Journal: Bioorg Med Chem Lett

Title: Amplification of DNA-binding affinities of protoberberine alkaloids by appended polyamines.

Authors: Pang JY, Long YH, Chen WH, Jiang ZH.

Abstract: This communication describes a synthetic approach toward the amplification of the moderate DNA-binding affinities of protoberberine alkaloids. Specifically, three protoberberine derivatives bearing two to six primary amino groups at the 3- and 9-positions of protoberberine were synthesized and characterized by NMR ((1)H and (13)C) and HRMS. Studies on their affinities toward calf thymus (CT) DNA by ethidium bromide (EB) displacement and spectrophotometric titration experiments indicate that these polyamino protoberberines show more than 10(3)-fold enhanced DNA-binding affinities relative to palmatine and thus are exploitable as strong DNA-binders.

CiteXplore: 17127054

DOI: 10.1016/j.bmcl.2006.11.037

Patent ID: