کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358914 | 981371 | 2015 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of novel indirubin-3′-monoxime derivatives as potent inhibitors against CDK2 and CDK9
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Discovery of novel indirubin-3′-monoxime derivatives as potent inhibitors against CDK2 and CDK9 Discovery of novel indirubin-3′-monoxime derivatives as potent inhibitors against CDK2 and CDK9](/preview/png/1358914.png)
چکیده انگلیسی
Indirubin-3′-monoxime (IM) is a potent cyclin-dependent kinase (CDK) inhibitor. Twenty novel IM derivatives were prepared to investigate the structure–activity relationships (SAR) of this compound class. Six compounds showed significant inhibition against both CDK2/cyclin E1 and CDK9/cyclin T1. The most potent compound 7t exhibited IC50 values at submicromolar level. Preliminary SAR trends were suggested and cytotoxicity of these compounds was investigated. Molecular docking studies on compounds 7l and 7t provided conducive clues for further structural optimization.
Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 11, 1 June 2015, Pages 2447–2451
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 11, 1 June 2015, Pages 2447–2451
نویسندگان
Lei Yan, Fangfang Lai, Xiaoguang Chen, Zhiyan Xiao,