2. Academic Validation
  3. Efficient synthesis and antiproliferative activity of novel thioether-substituted flavonoids

Efficient synthesis and antiproliferative activity of novel thioether-substituted flavonoids

  • Eur J Med Chem. 2013 Aug:66:161-70. doi: 10.1016/j.ejmech.2013.05.037.
Wei Huang 1,  Qiong Chen,  Wen-Chao Yang,  Guang-Fu Yang
Affiliations

Affiliation

  • 1 Key Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, PR China.
PMID: 23792763 DOI: 10.1016/j.ejmech.2013.05.037
Abstract

As widely occurring Natural Products, Flavonoids are an important source for drug discovery, due to their structural diversity and broad-spectrum biological activity. In this work, a library of novel, thioether-substituted Flavonoids with diverse heterocyclic groups was synthesized via a microwave-assisted procedure with the advantages of good yields, short times, mild conditions and ready isolation of the products. Their antiproliferative activities were evaluated against six Cancer cell lines, HCCLM-7, Hela, MDA-MB-435S, SW-480, Hep-2, and MCF-7 by the MTT-based assay. Compared with the positive control 5-fluorouracil, three compounds, 6a, 6b and 6j were successfully identified as the most promising candidates, due to their higher potency and broad-spectrum bioactivity with IC50 values in the range of 0.43 μM-6.7 μM.

Keywords

Antiproliferative activity; Chromone; Flavonoids; Microwave-assisted synthesis; Thioether.

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