کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370569 | 981822 | 2015 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of 2-arylamino-4-(1-methyl-3-isopropylsulfonyl-4-pyrazol-amino)pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors
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
چکیده انگلیسی
A new series of 2,4-diamino pyrimidine derivatives with a sulfone-substituted pyrazole right side-chain were discovered as potent anaplastic lymphoma kinase inhibitors. Structure–activity relationship of the left side-chain on phenyl substitutions were explored which delivered many potent ALK inhibitors. Among them, 29a showed favorable pharmacokinetic profiles in rats and dogs together with significant antitumor efficacy in EML4-ALK fusion xenograft model.
Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 17, 1 September 2015, Pages 3738–3743
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 17, 1 September 2015, Pages 3738–3743
نویسندگان
Peilong Zhang, Jiaqiang Dong, Boyu Zhong, Deyi Zhang, Can Jin, Xuejing Meng, Desheng Sun, Xiangyuan Xu, Yong Zhou, Zhi Liang, Minghua Ji, Hailong Li, Tao Xu, Guowei Song, Ling Zhang, Gang Chen, Hongbin Yuan, Joe Shih, Ruihao Zhang, Guojun Hou, Ying Jin,