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Article

Development of Furanopyrimidine-Based Orally Active Third-Generation EGFR Inhibitors for the Treatment of Non-Small Cell Lung Cancer.

Journal of medicinal chemistry - 23 Feb 2023

Li Mu-Chun, Coumar Mohane Selvaraj, Lin Shu-Yu, Lin Yih-Shyan, Huang Guan-Lin, Chen Chun-Hwa, Lien Tzu-Wen, Wu Yi-Wen, Chen Yen-Ting, Chen Ching-Ping, Huang Yu-Chen, Yeh Kai-Chia, Yang Chen-Ming, Kalita Bikashita, Pan Shiow-Lin, Hsu Tsu-An, Yeh Teng-Kuang, Chen Chiung-Tong, Hsieh Hsing-Pang

Abstract excerpt

The development of orally bioavailable, furanopyrimidine-based double-mutant (L858R/T790M) EGFR inhibitors is described. First, selectivity for mutant EGFR was accomplished by replacing the (S)-2-phenylglycinol moiety of 12 with either an ethanol or an alkyl substituent. Then, the cellular potency and physicochemical properties were optimized through insights from molecular modeling studies by implanting various...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 36749735
DOI: 10.1021/acs.jmedchem.2c01434
PMCID: PMC9969398

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