Synthesis, cytotoxicity and antitumor activity of 2,3-Diarylcy-clopent-2-ene-1-ones
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 series3 exhibited the most potent cytotoxicity with 3-aryl ring being 4-methoxyphenyl (compound3f), (3-hydroxy-4-methoxy)phenyl (compound3e), or (3-amino-4-methoxy)phenyl (compound3j).
Key words2,3-Diarylcyclopent-2-ene-1-ones Cytotoxicity Antitumor activity
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