Structure-activity relationship study of gatastatin based on the TOPLISS tree approach

Ichiro Hayakawa, Shuya Shioda, Takumi Chinen, Takeo Usui, Hideo Kigoshi

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)


- Various analogues of gatastatin, a y-tubulin-specific inhibitor, were designed and synthesized by systematically optimizing the aromatic ring at the 07-benzyl group in accordance with an operational Topliss tree, and their biological activities were evaluated. Some derivatives showed stronger cytotoxicity against HeLa cells than gatastatin. Especially, the cytotoxicity of the meta-chloro derivative was about 18-fold stronger than that of gatastatin. However, these derivatives did not exhibit binding ability to the yeast y-tubulin small complex or inhibitory activity against a,ß-tubulin polymerization. These results suggested that y-tubulin strongly recognized the unsubstituted phenyl ring of the 07-benzyl group in gatastatin.

Original languageEnglish
Pages (from-to)238-247
Number of pages10
Issue number1
Publication statusPublished - 2019

ASJC Scopus subject areas

  • Analytical Chemistry
  • Pharmacology
  • Organic Chemistry


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