Synthesis, Biological Evaluation and DNA Binding Properties of Novel Bleomycin Analogues
Bioorganic & Medicinal Chemistry Letters 13 (2003) 2595-2599，-0001，（）：
Aseries 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-DNAand cleavage efficiency to pBR322 DNAwere investigated, the results indicate that there is a positive relationship between DNAcleavage 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.
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