A number of 2,3-diarylquinol. derivatives were synthesized and evaluded for antiproliferative activities against the growth of six cancer cell lines including human hepatocelluar carcinoma (Hep G2 and Hep 3B), non-small cell lung cancer (A549 and Hl299), 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 more active than Tamoxifene against the growth of Hep 3B, H1299, and MDA-MB-231 with GI50 values of 0.71, 1.46, and 0.72 M respectively. Further investigations have shown that 16b induce cell cycle arrest at G2/M phase in a concentration-and time-dependent manner, DNA fragmentation, and disrupt the microtubule network in MDA-MB-231 cells. The apoptotic induction vas related to increase in the protein expressions of Bad and Bax and decrease in Bcl-2.
