Identification of acylthiourea derivatives as potent Plk1 PBD inhibitors
详细信息 查看全文
- 作者：Taikangxiang Yuna ; Tan Qinb ; Ying Liua ; b ; liuying@pku.edu.cn" class="auth_mail" title="E-mail the corresponding author ; Luhua Laia ; b ; c ; lhlai@pku.edu.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：Polo-like kinase 1 ; Polo-box domain ; Small molecular inhibitor ; Halogenosulfamoylphenyl acylthiourea ; Binding affinity ; In vitro assay
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：29 November 2016
- 年：2016
- 卷：124
- 期：Complete
- 页码：229-236
- 全文大小：1751 K
文摘
- •
A series of acylthioureas were designed and synthesized as Plk1 inhibitors.
- •
Compounds with halogen in sulfamoylphenyl group showed better binding affinities.
- •
The best compound 3v binds to Plk1 PBD with a Kd of 2.3 ± 0.1 μM.
- •
Compound 3v also inhibits the kinase activity of full-length Plk1.