کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10593748 | 981813 | 2012 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Anti-tumor activity of new orally bioavailable 2-amino-5-(thiophen-2-yl)benzamide-series histone deacetylase inhibitors, possessing an aqueous soluble functional group as a surface recognition domain
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
New orally bioavailable 5-(thiophen-2-yl)-substituted 2-aminobenzamide-series histone deacetylase inhibitors were synthesized. These compounds possess a morpholine or piperadine-derived moiety as an aqueous soluble functional group. Among them, 8b, having a 4-ethyl-2,3-dioxopiperazine-1-carboxamide group as a surface recognition domain, showed promising inhibitory activities against HCT116 cell growth and HDAC1/2. Notably, unlike MS-275, this compound did not induce apoptosis in the cell cycle tests. We therefore conducted antitumor tests of 8b and MS-275 against HCT116 cell xenografts in nude mice. Compound 8b reduced the volume of tumor mass to T/C: 60% and 47% at 45 and 80Â mg/kg over 16Â days, respectively. These values were comparable to the rate (T/C: 51% at 45Â mg/kg) for MS-275. Furthermore, 8b, at neither 45 nor 80Â mg/kg, induced the weight loss which was observed in the mice given MS-275 at 45Â mg/kg.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 5, 1 March 2012, Pages 1926-1930
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 5, 1 March 2012, Pages 1926-1930
نویسندگان
Yoshiyuki Hirata, Masahiko Hirata, Yasuyuki Kawaratani, Makio Shibano, Masahiko Taniguchi, Masahide Yasuda, Yoshiro Ohmomo, Yasuo Nagaoka, Kimiye Baba, Shinichi Uesato,