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  • Title: Synthesis and antiproliferative evaluation of 2,3-diarylquinoline derivatives.
    Author: Tseng CH, Chen YL, Chung KY, Wang CH, Peng SI, Cheng CM, Tzeng CC.
    Journal: Org Biomol Chem; 2011 May 07; 9(9):3205-16. PubMed ID: 21423988.
    Abstract:
    A number of 2,3-diarylquinoline derivatives were synthesized and evaluated for antiproliferative activities against the growth of six cancer cell lines including human hepatocellular carcinoma (Hep G2 and Hep 3B), non-small cell lung cancer (A549 and H1299), and breast cancer (MCF-7 and MDA-MB-231) cell lines. The preliminary results indicated that 6-fluoro-2,3-bis{4-[2-(piperidin-1-yl)ethoxy]phenyl}quinoline (16b) was one of the most active compounds against the growth of Hep 3B, H1299, and MDA-MB-231 with a GI(50) value of 0.71, 1.46, and 0.72 μM respectively which was more active than tamoxifen. Further investigations have shown that 16b induced cell cycle arrest at G2/M phase followed by DNA fragmentation via an increase in the protein expression of Bad, Bax and decrease in Bcl-2, and PARP which consequently cause cell death.
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