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Article

Discovery of novel spiro compound as RAF kinase inhibitor with in vitro potency against KRAS mutant cancer.

Bioorganic & medicinal chemistry letters - 1 May 2022

Zhao Peng, Wang Xiangzhu, Zhuang Linghang, Huang Song, Zhou Yu, Yan Yuna, Shen Ru, Zhang Fan, Li Jie, Hu Qiyue, Liu Suxing, Zhang Rumin, Dong Ping, Wan Hong, Bai Chang, He Feng, Tao Weikang

Abstract excerpt

The development of RAF inhibitors targeting cancers with wild type RAF kinase and/or RAS mutation has been challenging due to the paradoxical activation of the RAS-RAF-MEK-ERK cascade following RAF inhibitor treatment. Herein is the discovery and optimization of a series of RAF inhibitors with a novel spiro structure. The most potent spiro molecule 9 showed excellent in vitro potency against b/c RAF enzymes and...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 35276360
DOI: 10.1016/j.bmcl.2022.128666

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026.

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