Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes

Hsueh Yun Lee, Chih Yi Chang, Mei Jung Lai, Hsun Yueh Chuang, Ching Chuan Kuo, Chi Yen Chang, Jang Yang Chang, Jing Ping Liou

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16 Citations (Scopus)


This study reports the synthesis of a series of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes, which are potent antitubulin agents. Compound 13, (2-hydroxy-3,4,5-trimethoxyphenyl)-(6-methoxy-1H-indol-3-yl)-methanone exhibits marked antiproliferative activity against KB and MKN45 cells with IC50 values of 8.8 and 10.5 nM, respectively, binds strongly to the colchicine binding site and leads to inhibition of tubulin polymerization. It also behaves as a vascular disrupting agent which suppresses the formation of capillaries. The C2-OH group in the A-ring of this compound not only retains the biological activity but has valuable physicochemical properties.

Original languageEnglish
Pages (from-to)4230-4236
Number of pages7
JournalBioorganic and Medicinal Chemistry
Issue number15
Publication statusPublished - 2015 Jul 23

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Lee, H. Y., Chang, C. Y., Lai, M. J., Chuang, H. Y., Kuo, C. C., Chang, C. Y., Chang, J. Y., & Liou, J. P. (2015). Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes. Bioorganic and Medicinal Chemistry, 23(15), 4230-4236.