Synthesis and biological evaluation of novel GSK-3β inhibitors as anticancer agents

Min Jeong Choi, Da Won Oh, Jae Wan Jang, Yong Seo Cho, Seon Hee Seo, Kyu Sung Jeong, Soo Young Ko, Ae Nim Pae

Research output: Contribution to journalArticlepeer-review

2 Scopus citations


A series of isoxazol-indolin-2-one was designed for GSK-3β inhibitors as novel anticancer agents based on their binding mode analysis in GSK-3β crystal structure. Total 21 compounds were synthesized and evaluated for their inhibitory activity against two tumor cell lines (DU145 and HT29). Most of the synthesized compounds were potent with above 80% inhibitory activity at 100 μM, and several compounds were examined for inhibitory activity against GSK-3β. Among them, 15(Z) (R1=H, R2=3-Cl-phenyl) was most active with 78% inhibition of tumor cell line (HT29) at 20 μM and 72% inhibition of GSK-3β at 20 μM.

Original languageEnglish
Pages (from-to)2015-2020
Number of pages6
JournalBulletin of the Korean Chemical Society
Issue number6
StatePublished - 20 Jun 2011


  • Anticancer
  • Glycogen synthase kinase 3β
  • Inhibitor
  • Isoxazol-indolin-2-one


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