Synthesis of selenophene derivatives as novel CHK1 inhibitors

✍ Scribed by Pao-Chiung Hong; Li-Jung Chen; Tzu-Yun Lai; Huei-Yu Yang; Shih-Jan Chiang; Yann-Yu Lu; Ping-Kuei Tsai; Hung-Yi Hsu; Win-Yin Wei; Chu-Bin Liao

• Book ID: 104004644
• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 391 KB
• Volume: 20
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.07.034

✦ Synopsis

A series of selenophene derivatives 3 were synthesized as potential CHK1 inhibitors. The effects of substitution on the 4'- or 5'-position of selenophene moiety and shifting the hydroxyl group position on C6- phenolic ring of oxindole were explored. This study led to the discovery of the most potent CHK1 inhibitors 29-33 and 39-43, which had IC(50) values in the subnanomolar range.