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ID: ALA1136142

Journal: Bioorg Med Chem Lett

Title: Synthesis, biological evaluation and DNA binding properties of novel bleomycin analogues.

Authors: Xu ZD, Wang M, Xiao SL, Liu CL, Yang M.

Abstract: A series of bleomycin analogues was prepared with a facile synthetic method. All the compounds were shown to display significant antitumor activity against HeLa and BGC-823 cell lines in vitro. The binding properties with CT-DNA and cleavage efficiency to pBR322 DNA were investigated, the results indicate that there is a positive relationship between DNA cleavage efficiency and the binding affinity to DNA, and the antitumor activity of the bleomycin analogues is enhanced as the hydrophobicity of the C-terminus substituent side chain increased.

CiteXplore: 12852974

DOI: 10.1016/s0960-894x(03)00435-9