Title of article :
Synthesis and antiproliferative evaluation of certain iminonaphtho[2,3-b]furan derivatives Original Research Article
Author/Authors :
Chih-Hua Tseng، نويسنده , , Yeh-Long Chen، نويسنده , , Sheng-Huei Yang، نويسنده , , Shin-I Peng، نويسنده , , Chih-Mei Cheng، نويسنده , , Chein-Hwa Han، نويسنده , , Shinne-Ren Lin، نويسنده , , Cherng-Chyi Tzeng، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2010
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.
Keywords :
antiproliferative activity , 3-b]furan derivatives , anticancer agents
Journal title :
Bioorganic and Medicinal Chemistry
Journal title :
Bioorganic and Medicinal Chemistry