Jing, Lanlan; Wu, Gaochan; Hao, Xia; Olotu, Fisayo A.; Kang, Dongwei; Chen, Chin Ho; Lee, Kuo-Hsiung; Soliman, Mahmoud E. S.; Liu, Xinyong; Song, Yuning; Zhan, Peng published their research in European Journal of Medicinal Chemistry on December 1 ,2019. The article was titled 《Identification of highly potent and selective Cdc25 protein phosphatases inhibitors from miniaturization click-chemistry-based combinatorial libraries》.Formula: C7H6Cl2 The article contains the following contents:
Cell division cycle 25 (Cdc25) protein phosphatases play key roles in the transition between the cell cycle phases and their association with various cancers has been widely proven, which makes them ideal targets for anti-cancer treatment. Though several Cdc25 inhibitors have been developed, most of them displayed low activity and poor subtype selectivity. Therefore, it is extremely important to discover novel small mol. inhibitors with potent activities and significant selectivity for Cdc25 subtypes, not only served as drugs to treat cancer but also to probe its mechanism in transitions. In this study, miniaturized parallel click chem. synthesis via CuAAC reaction followed by in situ biol. screening were used to discover selective Cdc25 inhibitors. The bioassay results showed that compound M2N12 proved to be the most potent Cdc25 inhibitor, which also act as a highly selective Cdc25C inhibitor and was about 9-fold potent than that of NSC 663284. Moreover, M2N12 showed remarkable anti-growth activity against the KB-VIN cell line, equivalent to that of PXL and NSC 663284. An all-atom mol. dynamics (MD) simulation approach was further employed to probe the significant selectivity of M2N12 for Cdc25C relative to its structural homologs Cdc25A and Cdc25B. Overall, above results make M2N12 a promising lead compound for further investigation and structural modification. After reading the article, we found that the author used 3-Chlorobenzylchloride(cas: 620-20-2Formula: C7H6Cl2)
3-Chlorobenzylchloride(cas: 620-20-2) has been used in the reaction of 3-methoxybenzyl chloride and ethyl 4-bromobenzoate in pure water, using zinc dust and a Pd catalyst.Formula: C7H6Cl2
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics