کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369391 | 981775 | 2013 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
A-ring modification of SCH 900229 and related chromene sulfone γ-secretase inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Attempts to block metabolism by incorporating a 9-fluoro substituent at the A-ring of compound 1 (SCH 900229) using electrophilic Selectfluor™ led to an unexpected oxidation of the A-ring to give difluoroquinone analog 1a. Oxidation of other related chromene γ-secretase inhibitors 2–8 resulted in similar difluoroquinone analogs 2a–8a, respectively. These quinone products exhibited comparable in vitro potency in a γ-scretase membrane assay, but were several fold less potent in a cell-based assay in lowering Aβ40–42, compared to their parent compounds.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 3, 1 February 2013, Pages 850–853
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 3, 1 February 2013, Pages 850–853
نویسندگان
Wen-Lian Wu, Thavalakulamgara K. Sasikumar, Martin S. Domalski, Li Qiang, Duane A. Burnett, John Clader, William J. Greenlee, Tze-Ming Chan, Julie Lee, Lili Zhang,