Journal of Medicinal Chemistry p. 4685 - 4700 (2020)
Update date:2022-07-29
Topics:
Huang, Pan
Le, Xiangyang
Huang, Fei
Yang, Jie
Yang, Haofeng
Ma, Junlong
Hu, Gaoyun
Li, Qianbin
Chen, Zhuo
Apcin is one of the few compounds that have been previously reported as a Cdc20 specific inhibitor, although Cdc20 is a very promising drug target. We reported here the design, synthesis, and biological evaluations of 2,2,2-trichloro-1-aryl carbamate derivatives as Cdc20 inhibitors. Among these derivatives, compound 9f was much more efficient than the positive compound apcin in inhibiting cancer cell growth, but it had approximately the same binding affinity with apcin in SPR assays. It is possible that another mechanism of action might exist. Further evidence demonstrated that compound 9f also inhibited tubulin polymerization, disorganized the microtubule network, and blocked the cell cycle at the M phase with changes in the expression of cyclins. Thus, it induced apoptosis through the activation of caspase-3 and PARP. In addition, compound 9f inhibited cell migration and invasion in a concentration-dependent manner. These results provide guidance for developing the current series as potential new anticancer therapeutics.
View MoreContact:+33-5-34012600
Address:28 ZA des Pignès
Jinan Jianfeng Chemical Co., Ltd
Contact:0086-531-88110457
Address:sales01(-a-t-)pharmachemm{dot}c+o+m
CGeneTech (Suzhou, China) Co., Ltd.
Contact:+86-512-62956962
Address:Room 101,Bld C11,218 Xinghu Rd.,Suzhou industrial Park
taicang liyuan chemical co,.ltd
website:http://www.tcliyuanchem.com/productse.php
Contact:86-512-53539583
Address:Room 804,Huaxu Building,No.95,Renmin South Road,Taicang city,Jiangsu Province,China
ShanDong XinDa Chemical CO.,LTD
Contact:086-0311-87580543
Address:No.168, High Technology Development Zone Jinan Shandong China
Doi:10.1039/b000996m
(2000)Doi:10.1007/s00044-010-9376-4
(2011)Doi:10.1211/146080800128736196
(2000)Doi:10.1016/S0968-0896(00)00148-6
(2000)Doi:10.1007/BF00758811
(1986)Doi:10.1021/jo01043a004
(1963)