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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis of selenophene derivatives as novel CHK1 inhibitors
Pao-Chiung Hong1, Li-Jung Chen, Tzu-Yun Lai
1Development Center for Biotechnology, Xizhi City, Taipei County, Taiwan. pchong@mail.dcb.org.tw
Bioorganic & Medicinal Chemistry Letters
|August 3, 2010
Abstract:
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.
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