کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375565 | 981941 | 2009 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: Design, synthesis, SAR studies, and in vivo antitumor activity
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A series of N-hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides were designed and synthesized as novel HDAC inhibitors. General SAR has been established for the substituents at positions 1 and 2, as well as the importance of the ethylene group and its attachment to position 5. Optimized compounds are much more potent than SAHA in both enzymatic and cellular assays. A representative compound, 23 (SB639), has demonstrated antitumor activity in a colon cancer xenograft model.
SAR has been established for R1, R2 and Z of benzimidazole-based HDAC inhibitors (XV). Compound 23 (SB639) is a promising lead for further optimization towards a clinical candidate.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 5, 1 March 2009, Pages 1403–1408
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 5, 1 March 2009, Pages 1403–1408
نویسندگان
Haishan Wang, Niefang Yu, Hongyan Song, Dizhong Chen, Yong Zou, Weiping Deng, Pek Ling Lye, Joyce Chang, Melvin Ng, Stéphanie Blanchard, Eric T. Sun, Kanda Sangthongpitag, Xukun Wang, Kee Chuan Goh, Xiaofeng Wu, Hwee Hoon Khng, Lijuan Fang, Siok Kun Goh,