Synthesis and antitumor evaluation of methyl spongoate analogs

Cheng Shi Jiang, Cai Guo Huang, Bo Feng, Jia Li, Jing Xu Gong, Tibor Kurtán, Yue Wei Guo

Research output: Contribution to journalArticle

20 Citations (Scopus)

Abstract

A series of novel methyl spongoate (1) analogs has been synthesized and evaluated for their in vitro cytotoxic properties. It was found that the nature of the C-20 side chain had significant effects on their bioactivities and some analogs showed higher cytotoxicity than 1 against A549, HCT-116, HepG2, SW-1990, MCF-7 and NCI-H460 tumor cell lines. The pharmacological results confirmed that the α,β-unsaturated carbonyl moiety, a Michael acceptor in ring A, plays a pivotal role in the cytotoxic effect of these derivatives. The compiled pharmacological data may be useful for the design of novel analogous anticancer drugs.

Original languageEnglish
Pages (from-to)1153-1163
Number of pages11
JournalSteroids
Volume75
Issue number13-14
DOIs
Publication statusPublished - Dec 12 2010

Keywords

  • Cytotoxicity
  • Methyl spongoate analogs
  • Michael acceptor
  • Synthesis

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Endocrinology
  • Pharmacology
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Jiang, C. S., Huang, C. G., Feng, B., Li, J., Gong, J. X., Kurtán, T., & Guo, Y. W. (2010). Synthesis and antitumor evaluation of methyl spongoate analogs. Steroids, 75(13-14), 1153-1163. https://doi.org/10.1016/j.steroids.2010.08.002