Synthesis, biological evaluation and molecular modeling studies of imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors
详细信息 查看全文
- 作者：Marie Lawsona ; Jordi Rodrigoa ; Blandine Baratteb ; Thomas Robertb ; Claire Delehouzé ; b ; Olivier Lozachb ; Sandrine Ruchaudb ; Sté ; phane Bachb ; Jean-Daniel Briona ; Mouad Alamia ; ; Abdallah Hamzea ; abdallah.hamze@u-psud.fr" class="auth_mail" title="E-mail the corresponding author
- 关键词：CLK1 ; DYRK1A ; Kinase inhibitors ; Imidazo[1 ; 2-a]pyridines
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：10 November 2016
- 年：2016
- 卷：123
- 期：Complete
- 页码：105-114
- 全文大小：2850 K
文摘
- •
Imidazo[1,2-a]pyridines 4 were synthesized in one step from 2-aminopyridines and 2-bromoacephenones in good yield.
- •
Six imidazo[1,2-a]pyridines derivatives were active on kinases with micromolar IC50. (0.7–8.9 μM).
- •
The most active imidazo[1,2-a]pyridines derivative 4c inhibits kinases with a IC50 of 0.7 μM (CLK1) and 2.6 μM (DYRKA1).
- •
Docking studies indicate that 4c good binding mode on CLK1 and DYRKA1.