Synthesis and antiproliferative evaluation of 6-aryl-11-iminoindeno[1,2-c]quinoline derivatives |
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| Authors: | Tseng Chih-Hua Tzeng Cherng-Chyi Chung Kuin-Yu Kao Chai-Lin Hsu Chih-Yao Cheng Chih-Mei Huang Keng-Shiang Chen Yeh-Long |
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| Affiliation: | aDepartment of Medicinal and Applied Chemistry, College of Life Science, and Center of Excellence for Environmental Medicine, Kaohsiung Medical University, Kaohsiung City 807, Taiwan;bDepartment of Biomedical Science and Environmental Biology, College of Life Science, and Center of Excellence for Environmental Medicine, Kaohsiung Medical University, Kaohsiung, Taiwan;cThe School of Chinese Medicine for Post-Baccalaureate, I-Shou University, Kaohsiung, Taiwan |
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| Abstract: | A number of 6-aryl-11-iminoindeno[1,2-c]quinoline derivatives were synthesized and evaluated for their antiproliferative activities. Among them, (E)-6-{4-[3-(dimethylamino)propoxy]phenyl}-2-fluoro-9-hydroxy-11H-indeno[1,2-c]quinolin-11-one O-3-(dimethylamino)propyl oxime (23a) was the most active, exhibited GI50 values of 0.64, 0.39, 0.55, 0.67, and 0.65 μM against the growth of Hep G2, Hep 3B, A549, H1299, and MDA-MB-231, respectively. Compound 23a inhibited the growth of hepatoma cell lines in a dose- and time-dependent manner. The proportion of cells was decreased in the G1 and accumulated in G2/M phase after 12 h treatment of 23a, while the hypodiploid (sub-G0/G1 phase) cells increased. Further investigations have shown that 23a induced cell cycle arrest at G2/M phase and induce apoptosis via activation of p53, Bax, and caspase-8 which consequently cause cell death. |
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| Keywords: | 6-Arylindeno[1,2-c]quinoline derivatives Antiproliferative activity Apoptotic induction |
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