Antitumor agents 295. E-ring hydroxylated antofine and cryptopleurine analogues as antiproliferative agents: Design, synthesis, and mechanistic studies

Xiaoming Yang, Qian Shi, Chin Yu Lai, Chi Yuan Chen, Emika Ohkoshi, Shuenn Chen Yang, Chih Ya Wang, Kenneth F. Bastow, Tian Shung Wu, Shiow Lin Pan, Che Ming Teng, Pan Chyr Yang, Kuo Hsiung Lee

研究成果: 雜誌貢獻文章

21 引文 斯高帕斯(Scopus)

摘要

Various E-ring hydroxylated antofine and cryptopleurine analogues were designed, synthesized, and tested against five human cancer cell lines. Interesting structure-activity relationship (SAR) correlations were found among these new compounds. The most potent compound 13b was further tested against a series of nonsmall cell lung cancer (NSCLC) cell lines in which it showed impressive antiproliferative activity. Mechanistic studies revealed that 13b is able to down-regulate HSP90 and β-catenin in A549 lung adenocarcinoma cells in a dose-dependent manner, suggesting a potential use for treating hedgehog pathway-driven tumorigenesis.
原文英語
頁(從 - 到)6751-6761
頁數11
期刊Journal of Medicinal Chemistry
55
發行號15
DOIs
出版狀態已發佈 - 八月 9 2012
對外發佈Yes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

指紋 深入研究「Antitumor agents 295. E-ring hydroxylated antofine and cryptopleurine analogues as antiproliferative agents: Design, synthesis, and mechanistic studies」主題。共同形成了獨特的指紋。

  • 引用此

    Yang, X., Shi, Q., Lai, C. Y., Chen, C. Y., Ohkoshi, E., Yang, S. C., Wang, C. Y., Bastow, K. F., Wu, T. S., Pan, S. L., Teng, C. M., Yang, P. C., & Lee, K. H. (2012). Antitumor agents 295. E-ring hydroxylated antofine and cryptopleurine analogues as antiproliferative agents: Design, synthesis, and mechanistic studies. Journal of Medicinal Chemistry, 55(15), 6751-6761. https://doi.org/10.1021/jm3001218