31478-45-2Relevant academic research and scientific papers
Discovery of a dual tubulin polymerization and cell division cycle 20 homologue inhibitor via structural modification on apcin
Huang, Pan,Le, Xiangyang,Huang, Fei,Yang, Jie,Yang, Haofeng,Ma, Junlong,Hu, Gaoyun,Li, Qianbin,Chen, Zhuo
, p. 4685 - 4700 (2020/06/08)
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.
(1, 1, 1-trichloro-2) carbamate derivative as well as preparation method and application thereof
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, (2020/09/12)
The invention relates to (1, 1, 1-trichloro-2) carbamate derivatives, and also relates to a preparation method and related medical application of the derivatives. The structural general formula of the(1, 1, 1-trichloro-2) carbamate derivative is shown as a formula (I-III). Compared with the prior art, the target compound provided by the invention is greatly enhanced in tumor inhibition activity compared with apcin, shows a good inhibition effect in a plurality of tumor cell strains, and has a good microtubule aggregation inhibition effect. Therefore, a new way is opened up for searching for adifunctional cancer treatment method aiming at APC pathway and microtubule inhibition.
