کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376042 | 981949 | 2007 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
N-(2-Amino-phenyl)-4-(heteroarylmethyl)-benzamides as new histone deacetylase inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A variety of N-(2-amino-phenyl)-4-(heteroarylmethyl)-benzamides were designed and synthesized. These compounds were shown to inhibit recombinant human HDAC1 with IC50 values in the sub-micromolar range. In human cancer cells growing in culture these compounds induced hyperacetylation of histones, induced the expression of the tumor suppressor protein p21WAF1/Cip1, and inhibited cellular proliferation. Certain compounds of this class also showed in vivo activity in various human tumor xenograft models in mice.
A variety of N-(2-amino-phenyl)-4-(heteroarylmethyl)-benzamides of general structure 10 were designed, synthesized, and evaluated as histone deacetylase (HDAC) inhibitors.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 24, 15 December 2007, Pages 6729–6733
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 24, 15 December 2007, Pages 6729–6733
نویسندگان
Arkadii Vaisburg, Isabelle Paquin, Naomy Bernstein, Sylvie Frechette, Frederic Gaudette, Silvana Leit, Oscar Moradei, Stephane Raeppel, Nancy Zhou, Giliane Bouchain, Soon Hyung Woo, Zhiyun Jin, Jeff Gillespie, James Wang, Marielle Fournel,