کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10590980 | 981734 | 2014 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Cytotoxic activity of butane type of 1,7-seco-2,7â²-cyclolignanes and apoptosis induction by Caspase 9 and 3
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
All stereoisomers of methoxybutane and fluorobutane type of 1,7-seco-2,7â²-cyclolignane were synthesized and cytotoxic activities of these compounds were compared with those of all stereoisomers of butane and butanol type compounds. Both enantiomers of butane type secocyclolignane showed higher cytotoxic activity (IC50 = 16-20 μM) than methoxy type compounds, whereas none was observed for all the stereoisomers of butanol type secocyclolignane, however, (â)-Kadangustin J showed stereospecific cytotoxic activity (IC50 = 47-67 μM). Since (R)-9â²-fluoro derivative 23 was most potent (IC50 = 19 μM) among the corresponding fluoro stereoisomers, (R)-9â²-alkyl derivatives were synthesized, hydrophobic 9â²-heptyl derivative 27 showing highest activity (IC50 = 3.7 μM against HL-60, IC50 = 3.1 μM against HeLa) in this experiment. Apoptosis induction caused by Caspase 3 and 9 for (R)-9â²-heptyl derivative 27 was observed in the research on the mechanism. A degradation of DNA into small fragments was also shown by DNA ladder assay.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 17, 1 September 2014, Pages 4231-4235
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 17, 1 September 2014, Pages 4231-4235
نویسندگان
Tuti Wukirsari, Hisashi Nishiwaki, Kosuke Nishi, Takuya Sugahara, Koichi Akiyama, Taro Kishida, Satoshi Yamauchi,