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- W2113247975 abstract "The isoflavones biochanin A (1a), genistein (1b), and daidzein (4) at concentrations >20 µM inhibit cell growth of various cancer cell lines. To enhance the antiproliferative activities of these compounds, we synthesized three analogs, 2-[3-carboxy-(6-tert-butoxycarbonylamino)-hexylamino-propyl]-7,5-dihydroxy-4′-methoxyisoflavone (3a), 2-[3-[N-[6-(tert-butoxycarbonyl)-aminohexyl]]-caboxamidopropyl]-5,7,4′-trihydroxyisoflavone (3b), and 5-{2-[3-(4-hydroxy-phenyl)-4-oxo-4H-chromen-7-yloxy]-acetylamino}-pentyl)-carbamic acid tert-butyl ester (6). When cancer cells expressing predominantly estrogen receptor mRNA of the β- relative to α-subtype were treated with 3a, 3b, or 6, DNA synthesis was inhibited in a dose-dependent manner, ranging from 15 to 3000 nmol/L, with little inhibitory effect in normal vascular smooth muscle cells. Compound 6 was the most potent one, and its antiproliferative effect in cancer cells was modulated by estrogen and by the apoptosis inhibitor Z-VADFK. When tested in vivo, compound 6 decreased tumor volume of ovarian xenografts by 50%, with no apparent toxicity. Compound 6 may be a promising agent for therapy of cancer either alone or in combination with chemotherapeutic agents." @default.
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- W2113247975 date "2007-11-09" @default.
- W2113247975 modified "2023-10-16" @default.
- W2113247975 title "Synthesis and Evaluation of the Antiproliferative Activities of Derivatives of Carboxyalkyl Isoflavones linked to N-t-Boc-hexylenediamine" @default.
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- W2113247975 doi "https://doi.org/10.1021/jm070727z" @default.
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