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Novel 2-Amino-1,4-Naphthoquinone Derivatives Induce A549 Cell Death through Autophagy.

ABSTRACT: A series of 1,4-naphthoquinone derivatives containing were synthesized as anti-cancer agents and the crystal structure of compound 5a was confirmed by X-ray diffraction. In addition, the inhibitory activities against four cancer cell lines (HepG2, A549, K562, and PC-3) were tested, respectively, and compound 5i showed significant cytotoxicity on the A549 cell line with the IC₅₀ of 6.15 μM. Surprisingly, in the following preliminary biological experiments, we found that compound 5i induced autophagy by promoting the recycling of EGFR and signal transduction in the A549 cell, resulting in the activation of the EGFR signal pathway. The potential binding pattern between compound 5i and EGFR tyrosine kinase (PDB ID: 1M17) was also identified by molecular docking. Our research paves the way for further studies and the development of novel and powerful anti-cancer drugs.

SUBMITTER: Tan HY

PROVIDER: S-EPMC10143525 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature

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Novel 2-Amino-1,4-Naphthoquinone Derivatives Induce A549 Cell Death through Autophagy.

Tan Hua-Yuan HY Liang Feng-Ming FM Zhang Wen-Jing WJ Zhang Yi Y Cui Jun-Hao JH Dai Yu-Yu YY Qiu Xue-Mei XM Wang Wen-Hang WH Zhou Yue Y Chen Dan-Ping DP Li Cheng-Peng CP

Molecules (Basel, Switzerland) 20230407 8

A series of 1,4-naphthoquinone derivatives containing were synthesized as anti-cancer agents and the crystal structure of compound 5a was confirmed by X-ray diffraction. In addition, the inhibitory activities against four cancer cell lines (HepG2, A549, K562, and PC-3) were tested, respectively, and compound 5i showed significant cytotoxicity on the A549 cell line with the IC50 of 6.15 μM. Surprisingly, in the following preliminary biological experiments, we found that c ...[more]

PMID: 37110525

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