Synthesis, cytotoxicity and antitumor activity of 2,3-diarylcyclopent-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 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).
Nam
Nguyen-Hai
NH
College of Pharmacy, Chungnam National University, Daejeon, Korea.
Kim
Yong
Y
You
Young-Jae
YJ
Hong
Dong-Ho
DH
Kim
Hwan-Mook
HM
Ahn
Byung-Zun
BZ
D000818:Animals; D003517:Cyclopentanes / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity*; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D006801:Humans; D051379:Mice
D003517:Cyclopentanes