Design, Synthesis, and Antitumor Activity of Erlotinib Derivatives

Overview

Journal Front Pharmacol

Date 2022 May 6

PMID 35517789

Authors

Long-Fei Mao

Zhen-Zhen Wang

Qiong Wu

Xiaojie Chen

Jian-Xue Yang

Xin Wang

Yue-Ming Li

Affiliations

Soon will be listed here.

Abstract

Nineteen erlotinib derivatives bearing different 1,2,3-triazole moieties were designed, synthesized, and evaluated for their potential against different cancer cell lines. The structures of the synthesized compounds were confirmed H NMR, C NMR, and HR MS. Preliminary antitumor activity assay results suggested that some compounds showed remarkable inhibitory activity against different cancer cell lines including the corresponding drug-resistant ones. Among these compounds, 3d was the most promising one with an IC of 7.17 ± 0.73 μM (KYSE70TR), 7.91 ± 0.61 μM (KYSE410TR), 10.02 ± 0.75 μM (KYSE450TR), 5.76 ± 0.3 3 μM (H1650TR), and 2.38 ± 0.17 μM (HCC827GR). A preliminary mechanism study suggested that compound 3d suppressed cancer cell proliferation through the EGFR-TK pathway.

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