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Synthesis and pharmacological evaluation of 2,3-diphenyl acrylonitriles-bearing halogen as selective anticancer agents.
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2018-05-31 , DOI: 10.1111/cbdd.13180 Jia-Jun Li 1 , Jun Ma 2 , Ya-Bing Xin 1 , Zhe-Shan Quan 1 , Yu-Shun Tian 1
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2018-05-31 , DOI: 10.1111/cbdd.13180 Jia-Jun Li 1 , Jun Ma 2 , Ya-Bing Xin 1 , Zhe-Shan Quan 1 , Yu-Shun Tian 1
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Eighteen novel 2,3-diphenyl acrylonitrile derivatives bearing halogens were designed, synthesized, and evaluated for biological activity. Preliminary in vitro results indicated that the majority of the compounds with a para-substituted halogen had considerable antiproliferative activity against five human cancer cell lines, including MGC-803, AGS, and BEL-7402, with IC50 values in the range of 0.46-100 μm. No significant toxic effects on the non-cancerous human liver cell line L-02 were observed. The selective inhibitory activities against cancer cells were significantly better than that of the control lead compound CA-4 and CA-4P. Particularly, potent activities were found for the derivatives of 3-(4-halogen phenyl)-2-(3,4,5-trimethoxyphenyl)acrylonitrile, such as 5c (4-fluoro), 5f (4-bromo), 5h (4-chloro), and 5k (4-trifluoro- methyl), for AGS with IC50 values of 0.75 ± 0.24, 0.68 ± 0.21, 0.41 ± 0.05, and 1.49 ± 0.92 μm, respectively. The antiproliferative effects of 5f were attributed to cell-cycle arrest in the G2 /M phase, induction of cellular apoptosis, suppression of cell migration, and inhibition of cell colony formation in AGS cells.
中文翻译：
含2,3-二苯基丙烯腈的卤素作为选择性抗癌剂的合成及药理评价。
设计，合成和评估了十八种带有卤素的新型2,3-二苯基丙烯腈衍生物。体外初步结果表明，大多数具有对位取代卤素的化合物对五种人类癌细胞系（包括MGC-803，AGS和BEL-7402）具有相当大的抗增殖活性，IC50值在0.46-100范围内微米 没有观察到对非癌性人肝细胞系L-02有明显的毒性作用。对癌细胞的选择性抑制活性明显优于对照铅化合物CA-4和CA-4P。特别是，发现了3-（4-卤代苯基）-2-（3,4,5-三甲氧基苯基）丙烯腈的衍生物，例如5c（4-氟），5f（4-溴），5h（ 4-氯）和5k（4-三氟甲基），对于IC50分别为0.75±0.24、0.68±0.21、0.41±0.05和1.49±0.92μm的AGS。5f的抗增殖作用归因于G2 / M期的细胞周期停滞，诱导细胞凋亡，抑制细胞迁移以及抑制AGS细胞中细胞集落形成。
更新日期：2018-05-31
中文翻译：
含2,3-二苯基丙烯腈的卤素作为选择性抗癌剂的合成及药理评价。
设计，合成和评估了十八种带有卤素的新型2,3-二苯基丙烯腈衍生物。体外初步结果表明，大多数具有对位取代卤素的化合物对五种人类癌细胞系（包括MGC-803，AGS和BEL-7402）具有相当大的抗增殖活性，IC50值在0.46-100范围内微米 没有观察到对非癌性人肝细胞系L-02有明显的毒性作用。对癌细胞的选择性抑制活性明显优于对照铅化合物CA-4和CA-4P。特别是，发现了3-（4-卤代苯基）-2-（3,4,5-三甲氧基苯基）丙烯腈的衍生物，例如5c（4-氟），5f（4-溴），5h（ 4-氯）和5k（4-三氟甲基），对于IC50分别为0.75±0.24、0.68±0.21、0.41±0.05和1.49±0.92μm的AGS。5f的抗增殖作用归因于G2 / M期的细胞周期停滞，诱导细胞凋亡，抑制细胞迁移以及抑制AGS细胞中细胞集落形成。
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