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Article

Design, synthesis and biological evaluation of novel macrocyclic derivatives bearing aniline pyrimidine scaffolds as EGFR-TKIs.

Bioorganic & medicinal chemistry letters - 1 Nov 2022

Shen Yuhui, Xiao Xiaofei, Zhang Peng, Wang Qiang, Zhu Xueyan, Yang Yulei, Chen Yinbo

Abstract excerpt

Based on EGFR-TKI Osimertinib as lead compound, a series of novel macrocyclic derivatives bearing aniline pyrimidine scaffolds were designed and synthesized by macrocyclization. Their structures were identified by 1H NMR, 13C NMR, 19F NMR and HRMS. The pharmacological activities of the target compounds were tested and the preliminary structure-activity relationship was discussed. Among them, 17-membered ring...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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PMID: 36064123
DOI: 10.1016/j.bmcl.2022.128970

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