Improving potency and metabolic stability by introducing an alkenyl linker to pyridine-based histone deacetylase inhibitors for orally available RUNX3 modulators

详细信息    查看全文

• 作者：Doona Song^a ; Chulho Lee^a ; Yoon Jeong Kook^a ; ^c ; Soo Jin Oh^b ; Jong Soon Kang^b ; Hyun-Jung Kim^a ; Gyoonhee Han^a ; ^c ; ^{gyoonhee@yonsei.ac.kr}
• 关键词：RUNX3 ; RUNX3 acetylation ; HDAC inhibition ; Epigenetic control ; Protein stabilization
• 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：997-1010
• 全文大小：1457 K
• 卷排序：126

文摘

A new series of RUNX3 modulators showed improved in vitro biological evaluations metabolic stability profiles. Compounds exhibited a significant in vivo antitumor activity and pharmacokinetic profiles. Compound 7k could be a highly potent and orally available anticancer agent.