4.5 Article

Discovery of an orally active antitumor agent that induces apoptosis and suppresses EMT through heat shock protein 90 inhibition

Journal

INVESTIGATIONAL NEW DRUGS
Volume 39, Issue 4, Pages 1179-1188

Publisher

SPRINGER
DOI: 10.1007/s10637-021-01083-9

Keywords

Chalcone; Proliferation; Hsp90; Apoptosis; Epithelial mesenchymal transition; In vivo

Funding

  1. key research and development projects of xuzhou science and technology council [KC16SL106]
  2. second military medical university [NKMI2019K07]

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HYQ97, a chalcone derivative, is a promising candidate for lung cancer treatment. It inhibits proliferation, degrades Hsp90, inhibits epithelial mesenchymal transition, induces apoptosis in lung cancer cell lines, and has significant inhibitory effects on tumor growth in vivo.
Background Nowadays, lung cancer seriously affects human health in the world. Therefore, it is of great significance to develop effective anti-lung cancer drugs. Methods In this work, chalcone derivative HYQ97 was designed via a molecular hybridization strategy. It was synthesized by the cycloaddition in the presence of sodium ascorbate under mild conditions. Lung cancer cell lines were cultured to investigate its antitumor effects in vitro and in vivo. ResultsHYQ97 inhibited the proliferation of lung cancer cell lines. Specifically, its IC50 value against lung cancer A549 cells was 74.26 nM. It could inhibit heat shock protein 90 (Hsp90) and degrade its client proteins in a dose-dependent manner. Furthermore, HYQ97 suppressed the epithelial mesenchymal transition process and induced apoptosis of A549 cells. Importantly, HYQ97 also had significant inhibitory effects on tumor growth in vivo. Conclusions Chalcone derivative HYQ97 is a promising candidate for lung cancer treatment.

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