2-Aroylquinoline-5,8-diones as potent anticancer agents displaying tubulin and heat shock protein 90 (HSP90) inhibition

Kunal Nepali, Sunil Kumar, Hsiang Ling Huang, Fei Chiao Kuo, Cheng Hsin Lee, Ching Chuan Kuo, Teng Kuang Yeh, Yu Hsuan Li, Jang Yang Chang, Jing Ping Liou, Hsueh Yun Lee

研究成果: Article同行評審

9 引文 斯高帕斯(Scopus)


This study reports the synthesis of a series of 2-aroylquinoline-5,8-diones (11-23) on the basis of scaffold hopping. The presence of a methoxy group at C6 assists the highly regioselective incorporation with various amines, and simplifies the structural identification process. Among the synthetic compounds, 6-dimethylamino-2-(3,4,5-trimethoxybenzoyl)-quinoline-5,8-dione (12) and 7-pyrrolidin-1-yl-2-(3,4,5-trimethoxybenzoyl)-quinoline-5,8-dione (23) exhibit remarkable anti-proliferative activity against the cancer cell lines tested with mean IC50 values of 0.14 and 0.27 μM, respectively. Compound 23 showed moderate inhibitory activity against tubulin polymerization with an IC50 value of 5.9 μM. In a western blot analysis, 23 caused induction of HSP70 and degradation of Akt, revealing that it possesses HSP90 inhibitory activity.

頁(從 - 到)716-723
期刊Organic and Biomolecular Chemistry
出版狀態Published - 2016 1月 1

All Science Journal Classification (ASJC) codes

  • 生物化學
  • 物理與理論化學
  • 有機化學


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