کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1357432 | 981251 | 2016 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and pharmacological evaluation of trifluoromethyl containing 4-(2-pyrimidinylamino)benzamides as Hedgehog signaling pathway inhibitors
ترجمه فارسی عنوان
سنتز و بررسی فارماکولوژیک تری فلوورمتییل حاوی 4- (2-پیریمیدینیلامین) بنزامید به عنوان مهار کننده های مسیر سیگنالینگ خارپشت
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
چکیده انگلیسی
In present study, a series of novel containing trifluoromethyl 4-(2-pyrimidinylamino)benzamide derivatives were designed by the fluorine scan strategy. Their Hh signaling inhibitory activities were evaluated by Gli-luciferase reporter method. The comprehensive SAR was discussed and several derivatives were found to display more potent Hh signaling inhibitory activity than positive drug vismodegib. Compound 13d was the most potent compound with IC50 of 1.44 nM against Hh signaling pathway and also exhibited optimal PK properties in the in vivo PK properties study, deserved as an ideal lead compound for further study in future.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 24, Issue 5, 1 March 2016, Pages 1079–1088
Journal: Bioorganic & Medicinal Chemistry - Volume 24, Issue 5, 1 March 2016, Pages 1079–1088
نویسندگان
Minhang Xin, Liandi Zhang, Jun Wen, Han Shen, Zhaoyu Liu, Xinge Zhao, Qiu Jin, Mengyu Wang, Lingfei Cheng, Wei Huang, Feng Tang,