Document Report Card

ID: ALA1122353

Journal: J Med Chem

Title: DNA binding studies of 7-bulky-substituted actinomycin analogues.

Authors: Brennan TF, Sengupta SK.

Abstract: The DNA binding properties of several 7-substituted aralkylaminoactinomycin D analogues have been studied by spectrophotometry, DNA melting temperature studies, DNA-drug dissociation studies, and circular dichroism. Despite the presence of such bulky groups as 2-pyrrolylmethylamino or 3,4-dichlorobenzylamino at the 7 position, these analogues bind to DNA, inhibit RNA synthesis, and exhibit antitumor activity. A model is proposed for the interaction of the pyrrolyl analogue with phosphate groups of the DNA binding site, explaining the increased binding affinity for DNA of this actinomycin D analogue.

CiteXplore: 6827565

DOI: 10.1021/jm00357a025