Chia Nan University of Pharmacy & Science Institutional Repository:Item 310902800/25397
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    Please use this identifier to cite or link to this item: https://ir.cnu.edu.tw/handle/310902800/25397


    Title: Synthesis and antiproliferative evaluation of certain iminonaphtho[2,3-b]furan derivatives
    Authors: Chih-Hua Tseng
    Yeh-Long Chen
    Sheng-Huei Yang
    Shin-I Peng
    Chih-Mei Cheng
    Chein-Hwa Han
    Shinne-Ren Lin
    Cherng-Chyi Tzeng
    Contributors: 藥學系
    Keywords: Iminonaphtho[2,3-b]furan derivatives
    Antiproliferative activity
    Anticancer agents
    Date: 2010-07
    Issue Date: 2012-06-05 10:10:36 (UTC+8)
    Abstract: Certain iminonaphtho[2,3-b]furan derivatives were synthesized from their respective carbonyl precursors in the regiospecific and the stereospecific manners. These compounds were evaluated for their antiproliferative effects against four human carcinoma cells (MCF7, NCI-H460, SF-268, and K562) and the normal fibroblast cell line (Detroit 551). Among them, (Z)-4-(hydroxyimino)naphtho[2,3-b]furan-9(4H)-one (8) and (Z)-4-methoxy-iminonaphtho[2,3-b]furan-9(4H)-one (9) exhibited GI50 values of 0.82 and 0.60 μM, respectively, against the growth of K562 cells and were inactive against the normal fibroblast Detroit 551. The selectivity index (SI) on K562 cell for 8 and 9 was >121.95 and >166.67, respectively, which is comparable to daunorubicin (SI = 239) and is more favorable than camptothecin (SI = 16.5). The cell cycle analysis on K562 indicated that these compounds arrest the cell cycle at the G2/M phase. The morphological assessment and DNA fragmentation analysis indicated that 9-induced cell apoptosis in K562 cells. The apoptotic induction may through caspase-3 activity and cleavage of PARP.
    Relation: Bioorganic and Medicinal Chemistry 18(14)：p.5172-5182
    Appears in Collections:[Dept. of Pharmacy] Periodical Articles

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