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    Please use this identifier to cite or link to this item: http://asiair.asia.edu.tw/ir/handle/310904400/4577


    Title: Antitumor agents. 258. Syntheses and evaluation of dietary antioxidant-taxoid conjugates as novel cytotoxic agents
    Authors: Kyoko Nakagawa-Goto;Koji Yamada;Seikou Nakamura;Tzu-Hsuan Chen;Po-Cheng Chiang;Kenneth F. Bastow;Shao-Chun Wang;Bill Spohn;Mien-Chie Hung;Fang-Yu Lee;Fang-Chen Lee;Kuo-Hsiung Lee
    Keywords: Conjugation;Paclitaxel;Antioxidant;Cytotoxicity
    Date: 2007-09
    Issue Date: 2009-11-27 13:56:54 (UTC+8)
    Publisher: Asia University
    Abstract: Various dietary antioxidants, including vitamins, flavonoids, curcumin, and a coumarin, were conjugated with paclitaxel (1) through an ester linkage. The newly synthesized compounds were evaluated for cytotoxic activity against several human tumor cell lines as well as the corresponding normal cell lines. Interestingly, most tested conjugates selectively inhibited the growth of 1A9 (ovarian) and KB (nasopharyngeal) tumor cells without activity against other cell lines. Particularly, conjugates 16 and 20 were highly active against 1A9 (ED50 value of 0.005 ?g/mL) as well as KB (ED50 values of 0.005 and 0.14 ?g/mL, respectively) cells. Compound 22b, the glycinate ester salt of vitamin E conjugated with 1, appears to be a promising lead for further development as a clinical trial candidate as it exhibited strong inhibitory activity against Panc-1 (pancreatic cancer) with less effect on the related E6E7 (normal) cell line.
    Relation: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 17(18):5204-5209
    Appears in Collections:[生物科技學系] 期刊論文

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