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Updated: Sep 28, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis, cytotoxicity and antitumor activity of 2,3-diarylcyclopent-2-ene-1-ones
Nguyen-Hai Nam1, Yong Kim, Young-Jae You
1College of Pharmacy, Chungnam National University, Daejeon, Korea.
Abstract:
Two series of 2,3-diarylcyclopent-2-ene-1-ones including 2-aryl-3-(2,5-dihydroxyphenyl)cyclopent-2-ene-1-ones (2a-2f) and 3-aryl-2-3',4',5'-trimethoxyphenyl)cyclopent-2-ene-1-one (3a-3j) were synthesized and evaluated for the cytotoxicity against three tumor cell lines; B16F10, HCT116 and A431. It was found that the 3,4,5-trimethoxy substituent was optimal for the bioactivity of compounds in series 2. Meanwhile, compounds in series 3 exhibited the most potent cytotoxicity with 3-aryl ring being 4-methoxyphenyl (compound 3f), (3-hydroxy-4-methoxy)phenyl (compound 3e), or (3-amino-4-methoxy)phenyl (compound 3j).
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