DNA-Binding Activity and Cytotoxicity of the Extended Diphenylfuran Bisamidines in Breast Cancer MCF-7 Cells

スポンサーリンク

概要

• 論文の詳細を見る

• The DNA binding properties of therr novel ectended diphenyulfuran bisamidines(1-3)possessing different dicationic terminal side chains were studied. The ultrafiltration assay showed that bisamidines 1-3 have significant affinity for DNA. The DNA-binding data for bisamidines 1-3 using homopolymers poly(dA-dT)・poly(dA-dT)and poly(dG-dC)・poly(dG-dC), indecated that these compounds show moderate specificity for AT base pairs.We studied the cytotoxicity effects of bisamidines 1-3, Hoechst 33258 and DAPI(4´, 6-diamidino-2-phenylindole)in gultured breast cancer MCF-7 cells. The bisamidines 1-3 showed comparable antitumour activity to Hoechst 33258, but were substantially more cytotoxic conpared to DAPI. These data show that in broad terms the cytotoxic potency of bisamidines 1-3 in cultured breast cancer MCF-7 cells decreased with the size of the alkyl group substituent(cyclopropyl>isopriopyl>cyclopentyl), 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
• 2001-06-01

著者

• Bielawska Anna

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

• Bielawska Anna

  Department Of Medicinal Chemistry And Drug Technology Medical Academy Of Bialystok

• Wolczynski S

  Department Of Gynecological Endocrinology Medical Academy Of Bialystok

• Wolczynski Slawomir

  Department Of Gynecological Endocrinology Medical Academy Of Bialystok

• BIEKAWSKI Krzysztof

  Department of Medicinal Chemistry and Drug Technology, Medical Academy of Bialystok

• Biekawski Krzysztof

  Department Of Medicinal Chemistry And Drug Technology Medical Academy Of Bialystok

• Bielawski Krysztof

  Department of Medicinal Chemistry and Drug Technology, Medical Academy of Bialystok

関連論文

• The Effect of Generation 2 and 3 Poly (amidoamine) Dendrimers on Viability of Human Breast Cancer Cells
• Antiproliferative Activity of Derivatives of Ouabain, Digoxin and Proscillaridin A in Human MCF-7 and MDA-MB-231 Breast Cancer Cells(Pharmacology)
• Inhibition of DNA Topoisomerases I and II, and Growth Inhibition of Breast Cancer MCF-7 Cells by Ouabain, Digoxin and Proscillaridin A(Pharmacology)
• 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
• DNA-Binding Activity and Cytotoxicity of the Extended Diphenylfuran Bisamidines in Breast Cancer MCF-7 Cells
• Modulation of Prolidase Activity during in Vitro Aging of Human Skin Fibroblasts the Role of Extracellular Matrix Collagen

スポンサーリンク