YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
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Synthesis of 2',4'-Dimethoxychalcone Derivatives and Evaluation of Their Antitumor Activities Against Non-small Cell Lung Cancer

2',4'-Dimethoxychalcone 유도체 합성 및 비소폐암세포주에서 항암 활성평가

  • Received : 2016.04.15
  • Accepted : 2016.05.10
  • Published : 2016.06.30
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Abstract

Heat shock protein 90 (Hsp90) is a ubiquitous molecular chaperone, which is associated with stabilization of many oncogenic proteins for cancer cell survival. Hsp90 is overexpressed 2-10 fold higher in cancer cells than normal cells. Due to its potential to simultaneously disable multiple signaling pathway, Hsp90 has been identified as a validated target for cancer therapy. Accordingly, we designed and synthesized 2',4'-dimethoxychalcone derivatives to inhibit Hsp90 chaperone function. Among 2',4'-dimethoxychalcone derivatives, we found that compound 1g disrupted Hsp90 chaperoning function and impaired the growth of cancer cells. These findings indicated that 1g could serve a potential lead compound to target Hsp90 in cancer chemotherapy.

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References

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