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Updated: Apr 17, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and structure-activity relationship studies of furan-ring fused chalcones as antiproliferative agents
Yusuke Saito1, Maho Kishimoto1, Yuko Yoshizawa2
1Laboratory of Bio-organic Chemistry, Tokyo Denki University, Hatoyama, Saitama, Japan.
Abstract:
As part of our continuing investigation of flavonoid derivatives as potential anticancer substances, the synthesis of 25 cinnamoyl derivatives of benzofuran as furan-fused chalcones was carried-out and these compounds were further evaluated for their antiproliferative activity towards HL60 promyelocytic leukemia cells. In comparison with 2',4'-dihydroxychalcone, attachment of a furan moiety on the A-ring enhanced activity by more than twofold. Benzofurans may be useful in the design of biologically active flavonoids.
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