Synthesis of flavonoid analogues as scaffolds for natural product-based combinatorial libraries

Nianhuan Yao, Aiming Song, Xiaobing Wang, Seth Dixon, Kit Lam

Research output: Contribution to journalArticlepeer-review

51 Scopus citations


The design and synthesis of flavonoid analogues as combinatorial scaffolds is reported. Using commercially available materials, we synthesized chalcones with fluoro and carboxy groups. Nitration of these compounds generated highly functionalized flavonoid scaffolds with an o-fluoronitrobenzene template. Subsequent cyclizations of these chalcones resulted in the formation of several flavone and flavonone scaffolds. One of the flavonones was chosen as the scaffold to synthesize flavonoid derivatives on the solid phase. A series of flavonoid derivatives were obtained in high yields, which demonstrates that these highly functionalized scaffolds can be used in the synthesis of natural product-based combinatorial libraries for drug discovery.

Original languageEnglish (US)
Pages (from-to)668-676
Number of pages9
JournalJournal of Combinatorial Chemistry
Issue number4
StatePublished - Jul 2007

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Discrete Mathematics and Combinatorics


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