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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antibiotics, Antineoplastic / chemical synthesis*
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Antibiotics, Antineoplastic / pharmacology
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Binding Sites / drug effects
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Bleomycin / analogs & derivatives*
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Bleomycin / chemical synthesis*
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Bleomycin / pharmacology
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Cell Line, Tumor
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Chemical Phenomena
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Chemistry, Physical
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Chromatography, Agarose
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DNA, Neoplasm / drug effects
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DNA, Neoplasm / metabolism*
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Drug Screening Assays, Antitumor
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HeLa Cells
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Humans
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Hydrogen-Ion Concentration
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Kinetics
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Magnetic Resonance Spectroscopy
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Tetrazolium Salts
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Thiazoles
Substances
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Antibiotics, Antineoplastic
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DNA, Neoplasm
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Tetrazolium Salts
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Thiazoles
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Bleomycin
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thiazolyl blue