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KMID : 0370220160600030135
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Yakhak Hoeji
2016 Volume.60 No. 3 p.135 ~ p.140
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Synthesis of 2’,4’-Dimethoxychalcone Derivatives and Evaluation of Their Antitumor Activities Against Non-small Cell Lung Cancer
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Choi Myeong-A
Jeong Ju-Hui
Oh Yong-Jin
Lee Young-Sook
Seo Yong-Ho
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Abstract
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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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KEYWORD
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chalcone, Hsp90, cancer, flavokawain B, small molecule
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