Synthesis of Novel 2,3-DiarylIquinoline Derivatives as Antiproliferative Agents

CNU IR > Pharmacy and Science > 2011 Taiwanese-Russian Organic, Medicinal and Bio Chemistry Interactions & PST Medicinal Chemistry Symposium > Item 310902800/24237

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Title:	Synthesis of Novel 2,3-DiarylIquinoline Derivatives as Antiproliferative Agents
Authors:	Wei-Fen Luo (羅偉棻) Chih-Hua Tseng (曾志華) Yeh-Long Chen (陳義龍) Kuin-Yu Chung (鍾昆宇) Chih-Mei Cheng (鄭智美) Chi-Huei Wang (王記慧) Cherng-Chyi Tzeng (曾誠齊)
Date:	2011
Issue Date:	2011-06-23 14:57:25 (UTC+8)
Abstract:	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.
Relation:	2011年台俄有機、藥物與生物化學交流暨藥物化學研討會，起迄日：2011/04/06~2011/04/05，地點：溪頭台大實驗林
Appears in Collections:	[Pharmacy and Science] 2011 Taiwanese-Russian Organic, Medicinal and Bio Chemistry Interactions & PST Medicinal Chemistry Symposium

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