Total Synthesis of Hispidulin and the Structural Basis for Its Inhibition of Proto-oncogene Kinase Pim-1

Shi Wei Chao, Ming Yuan Su, Lih Chu Chiou, Liang Chieh Chen, Chung I. Chang, Wei Jan Huang

Research output: Contribution to journalArticlepeer-review

14 Citations (Scopus)

Abstract

(Figure Presented). A new method is applied to synthesize hispidulin, a natural flavone with a broad spectrum of biological activities. Hispidulin exhibits inhibitory activity against the oncogenic protein kinase Pim-1. Crystallographic analysis of Pim-1 bound to hispidulin reveals a binding mode distinct from that of quercetin, suggesting that the binding potency of flavonoids is determined by their hydrogen-bonding interactions with the hinge region of the kinase. Overall, this work may facilitate construction of a library of hispidulin-derived compounds for investigating the structure-activity relationship of flavone-based Pim-1 inhibitors.

Original languageEnglish
Pages (from-to)1969-1976
Number of pages8
JournalJournal of Natural Products
Volume78
Issue number8
DOIs
Publication statusPublished - Aug 28 2015

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology
  • Pharmaceutical Science
  • Analytical Chemistry
  • Organic Chemistry
  • Molecular Medicine
  • Complementary and alternative medicine

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