Synthesis, DNA-Binding Activity and Cytotoxicity of Carbamate Derivatives of Hoechst 33258 in Breast Cancer MCF-7 Cells

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概要

• 論文の詳細を見る

• A series of carbamate derivatives of Hoechst 33258 was prepared as potential anticancer agents. These new compounds (l-4) were readily prepared in good yields by addition of chloroethyl, bromoethyl, chloropropyl or 4-(chloromethyl)phenyl isocyanates to Hoechst 33258. Their cytotoxic activity was evaluated on human breast cancer MCF-7. Compounds 1-4 were more cytotoxic than Hoechst 33258. In particular derivative 4, the most active of the series, is up to 3 times more potent than Hoechst 33258. The DNA-binding ability of these compounds was evaluated by an ultrafiltration method using calf thymus DNA. These data show that in broad terms the cytotoxic potency of 1-4 in cultured breast cancer MCF-7 cells increases, in accord with their increases in DNA affinity, as shown by the binding constant values.

• 公益社団法人日本薬学会の論文
• 2002-07-01

著者

• Bielawski Krzysztof

  Department Of Medicinal Chemistry And Drug Technology Faculty Of Pharmacy Medical University Of Bial

• Bielawska Anna

  Department of Medicinal Chemistry and Drug Technology, Faculty of Pharmacy Medical University of Bia

• WOLCZYNSKI Slawomir

  Department of Gynecological Endocrinology, Medical University of Bialystok

• Bielawska Anna

  Department Of Medicinal Chemistry And Drug Technology Faculty Of Pharmacy Medical University Of Bial

• Wolczynski Slawomir

  Department Of Gynecological Endocrinology Medical Academy Of Bialystok

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• Synthesis, DNA Binding, Topoisomerase Inhibition and Cytotoxic Properties of 2-Chloroethylnitrosourea Derivatives of Hoechst 33258(Medicinal Chemistry)
• Synthesis, DNA-Binding Activity and Cytotoxicity of Carbamate Derivatives of Hoechst 33258 in Breast Cancer MCF-7 Cells
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