Chia Nan University of Pharmacy & Science Institutional Repository:Item 310902800/25397
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    標題: Synthesis and antiproliferative evaluation of certain iminonaphtho[2,3-b]furan derivatives
    作者: Chih-Hua Tseng
    Yeh-Long Chen
    Sheng-Huei Yang
    Shin-I Peng
    Chih-Mei Cheng
    Chein-Hwa Han
    Shinne-Ren Lin
    Cherng-Chyi Tzeng
    貢獻者: 藥學系
    關鍵字: Iminonaphtho[2,3-b]furan derivatives
    Antiproliferative activity
    Anticancer agents
    日期: 2010-07
    上傳時間: 2012-06-05 10:10:36 (UTC+8)
    摘要: 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.
    显示于类别:[藥學系(所)] 期刊論文


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