期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 5, 页码 2112-2124出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm201344a
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资金
- UNIMITT of University of Milan, Italy
- University of Milano-Bicocca, Italy
- [2007K29W5J]
- [2009KFMP7Z]
A series of novel 1,4-diaryl-2-azetidinones were synthesized and evaluated for antiproliferative activity, cell cycle effects, and apoptosis induction. Strong cytotoxicity was observed with the best compounds (+/-)-trans-20, (+/-)-trans-21, and enantiomers (+)-trans-20 and (+)-trans-21, which exhibited IC50 values of 3-13 nM against duodenal adenocarcinoma cells. They induced inhibition of tubulin polymerization and subsequent G2/M arrest. This effect was accompanied by activation of AMP-activated protein kinase (AMPK), activation of caspase-3, and induction of apoptosis. Additionally, the most potent compounds displayed antiproliferative activity against different colon cancer cell lines, opening the route to a new class of potential therapeutic agents against colon cancer.
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