Structure-based design and synthesis of imidazo[1,2-a]pyridine derivatives as novel and potent Nek2 inhibitors with in vitro and in vivo antitumor activities

详细信息    查看全文

• 作者：Jian-Bei Xi^a ; ¹ ; Yan-Fen Fang^a ; ¹ ; Brendan Frett^b ; ¹ ; Meng-Li Zhu^a ; Tong Zhu^a ; Yan-Nan Kong^a ; Feng-Jie Guan^a ; Yun Zhao^a ; Xiong-Wen Zhang^a ; ^{xwzhang@sat.ecnu.edu.cn} ; Hong-yu Li^b ; ^HLi2@uams.ed ; Ming-Liang Ma^a ; ^{mlma@brain.ecnu.edu.cn} ; Wenhao Hu^a ; ^{whu@chem.ecnu.edu.cn}
• 关键词：Nek2 inhibitors ; Imidazo[1 ; 2-a]pyridine ; Antitumor activity ; Selectivity
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：1083-1106
• 全文大小：2794 K
• 卷排序：126

文摘

A series of novel and potent Nek2 inhibitors based on a new imidazo[1,2-a]pyridine scaffold were designed and synthesized. MBM-17 and MBM-55 effectively inhibited the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S and MBM-55S showed good selectivity and in vitro and in vivo antitumor activity without apparent toxicity.