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Updated: Sep 11, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Structure-activity relationship study of HIF-2α inhibitors with tricyclic scaffold
Zhijie Wu1, Changwei Chen1, Jian Yan1
1Kind Pharmaceuticals LLC, 126 Xinzhou Road, Hangzhou, Zhejiang Province 311100, China.
None:
HIF-2α is a member of the HIF transcription factor family and a key oncogenic driver in renal cell carcinoma, which is characterized by the overaccumulation of HIF-2α protein. Therefore, inhibition of HIF-2α holds therapeutic potential for renal cell carcinoma. Disclosed herein are the discovery and characterization of a novel series of HIF-2α inhibitors with a tricyclic scaffold. A systematic SAR study was performed, and optimization of the tricyclic scaffold demonstrated that a fluorine atom in the cis.
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