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

Research output: Contribution to journalArticle

21 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)6751-6761
Number of pages11
JournalJournal of Medicinal Chemistry
Volume55
Issue number15
DOIs
Publication statusPublished - Aug 9 2012
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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  • Cite this

    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