Synthesis and antiproliferative evaluation of certain iminonaphtho[2,3-b]furan derivatives

doi:10.1016/j.bmc.2010.05.062

Chia Nan University of Pharmacy & Science Institutional Repository > 藥理學院 > 藥學系(所) > 期刊論文 > 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.
關聯:	Bioorganic and Medicinal Chemistry 18(14)：p.5172-5182
顯示於類別:	[藥學系(所)] 期刊論文

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