Design, synthesis, and mechanism of action of 2-(3-hydroxy-5-methoxyphenyl) -6-pyrrolidinylquinolin-4-one as a potent anticancer lead

Yung Yi Cheng, Chin Yu Liu, Meng Tung Tsai, Hui Yi Lin, Jai Sing Yang, Tian Shung Wu, Sheng Chu Kuo, Li Jiau Huang, Kuo Hsiung Lee

研究成果: Article同行評審

7 引文 斯高帕斯(Scopus)

摘要

New 6- (or 6,7-) substituted 2-(hydroxyl substituted phenyl)quinolin-4-one derivatives were synthesized and screened for antiproliferative effects against cancer cell lines. Structure-activity relationship correlations were established and the most promising compound 2-(3-hydroxy-5-methoxyphenyl)-6-pyrrolidin-1- ylquinolin-4-one (6h) exhibited strong inhibitory activity against various human cancer cell lines, particularly non-small cell lung cancer NCI-H522. Additional studies suggested a mechanism of action resembling that of the antimitotic drug vincristine. The presence of a C-ring OH group in 6h will allow this compound to be converted readily to a water soluble and physicochemically stable hydrophilic prodrug. Compound 6h is proposed as a new anticancer lead compound.

原文English
頁(從 - 到)5223-5227
頁數5
期刊Bioorganic and Medicinal Chemistry Letters
23
發行號18
DOIs
出版狀態Published - 2013 九月 15

All Science Journal Classification (ASJC) codes

  • 生物化學
  • 分子醫學
  • 分子生物學
  • 藥學科學
  • 藥物發現
  • 臨床生物化學
  • 有機化學

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