Molecules, Vol. 24, Pages 4138: Potent Cytotoxicity of Novel L-Shaped Ortho-Quinone Analogs through Inducing Apoptosis
Molecules, Vol. 24, Pages 4138: Potent Cytotoxicity of Novel L-Shaped Ortho-Quinone Analogs through Inducing Apoptosis
Molecules doi: 10.3390/molecules24224138
Authors:
Sheng-You Li
Ze-Kun Sun
Xue-Yi Zeng
Yue Zhang
Meng-Ling Wang
Sheng-Cao Hu
Jun-Rong Song
Jun Luo
Chao Chen
Heng Luo
Wei-Dong Pan
Twenty-seven L-shaped ortho-quinone analogs were designed and synthesized using a one pot double-radical synthetic strategy followed by removing methyl at C-3 of the furan ring and introducing a diverse side chain at C-2 of the furan ring. The synthetic derivatives were investigated for their cytotoxicity activities against human leukemia cells K562, prostate cancer cells PC3, and melanoma cells WM9. Compounds TB1, TB3, TB4, TB6, TC1, TC3, TC5, TC9, TC11, TC12, TC14, TC15, TC16, and TC17 exhibited a better broad-spectrum cytotoxicity on three cancer cells. TB7 and TC7 selectively displayed potent inhibitory activities on leukemia cells K562 and prostate cancer cells PC3, respectively. Further studies indicated that TB3, TC1, TC3, TC7, and TC17 could significantly induce the apoptosis of PC3 cells. TC1 and TC17 significantly induced apoptosis of K562 cells. TC1, TC11, and TC14 induced significant apoptosis of WM9 cells. The structure-activity relationships evaluation showed that removing methyl at C-3 of the furan ring and introducing diverse side chains at C-2 of the furan ring is an effective strategy for improving the anticancer activity of L-shaped ortho...
Source: Molecules - Category: Chemistry Authors: Sheng-You Li Ze-Kun Sun Xue-Yi Zeng Yue Zhang Meng-Ling Wang Sheng-Cao Hu Jun-Rong Song Jun Luo Chao Chen Heng Luo Wei-Dong Pan Tags: Article Source Type: research
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