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Design, Synthesis, and Antitumor Activity of Erlotinib Derivatives.

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 via ¹H NMR, ¹³C 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 IC₅₀ 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.

SUBMITTER: Mao LF

PROVIDER: S-EPMC9065260 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature

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Design, Synthesis, and Antitumor Activity of Erlotinib Derivatives.

Mao Long-Fei LF Wang Zhen-Zhen ZZ Wu Qiong Q Chen Xiaojie X Yang Jian-Xue JX Wang Xin X Li Yue-Ming YM

Frontiers in pharmacology 20220420

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 via 1H NMR, 13C 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 thes ...[more]

PMID: 35517789

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