Synthesis and biological evaluation of α-methyl-chalcone for anticervical cancer activity
Synthesis and biological evaluation of α-methyl-chalcone for anticervical cancer activity
复制标题
α-甲基查尔酮的合成及抗宫颈癌活性的生物学评价
DOI：
10.1007/s00044-017-1891-0
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发表时间：
2017-09-01
影响因子：
2.6
通讯作者：
Yang, Zheng
中科院分区：
文献类型：
--
作者：
Ren, Bing-zhao;Ablise, Mourboul;Yang, Zheng
合成了一系列31个查尔酮化合物，并评价了它们对人宫颈癌细胞株(HeLa和SiHA)的抗增殖活性。化合物19，(E)-1-(2，4-dihydroxyphenyl)-3-(4-(dimethylamino)phenyl)-2-methylprop-2-en-1-one对HeLa和SiHa细胞有明显的抑制增殖作用(IC_(50)=0.035 mU·M)。Annexin V-FITC(异硫氰酸荧光素)/碘化丙啶(PI)染色显示，化合物19呈剂量依赖性增加细胞凋亡率。化合物19的分子模拟研究表明，最有效的结构停靠在酵母20 S蛋白酶体结合部位(蛋白质数据库代码-3E47)，并通过各种疏水和氢键作用稳定在空腔中。
A series of 31 chalcones were synthesized and evaluated for anti-proliferative activity against the human cervical cancer cell lines (HeLa and SiHa). Compound 19, (E)-1-(2,4-dihydroxyphenyl)-3-(4-(dimethylamino)phenyl)-2-methylprop-2-en-1-one was found to be an effective anti-proliferative agent in HeLa and SiHa cells (IC50 = 0.035 mu M). Compound 19 increased the percentage of apoptosis in a dose-dependent manner, as measured by Annexin V-FITC (fluorescein isothiocyanate)/(propidium iodide) PI staining. Molecular modeling studies of compound 19 showed that the most potent structure was docked at the yeast 20 S proteasome binding site (Protein Data Bank code-3E47) and was stabilized in the cavity by various hydrophobic and hydrogen bonding interactions.