In this section, you can access to the latest technical information related to the FUTURE project topic.

Discovery of 6,7-dihydro-5H-pyrrolo[3,4-d] pyrimidine derivatives as a new class of ATR inhibitors

Ataxia telangiectasia and Rad3-related (ATR) kinase is a key regulating protein within the DNA damage response (DDR), responsible for sensing replication stress (RS), and has been considered as a potential target for cancer therapy. Herein, we report the discovery of a series of 6,7-dihydro-5H-pyrrolo[3,4-d]-pyrimidine derivatives as a new class of ATR inhibitors. Among them, compound 5g exhibits an IC50 value of 0.007??M against ATR kinase. In vitro, 5g displays good anti-tumor activity and could significantly reduce the phosphorylation level of ATR and its downstream signaling protein. Overall, this study provides a promising lead compound for subsequent drug discovery targeting ATR kinase.

» Author: Pei Chen, Huachao Bin, Yan Jiao, Guifeng Lin, Yun Zhang, Anjie Xia, Zhilin Pan, Jingxin Qiao, Yinping Guo, Jingming Liu, Yangli Zhou, Linli Li

» Publication Date: 01/05/2022

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