含香豆素部分的新型苯并降冰片烯酮结构单元的合成及其作为潜在抗癌剂的评估。
Synthesis of novel building blocks of benzosuberone bearing coumarin moieties and their evaluation as potential anticancer agents.
作者信息
Yadagiri Bandi, Holagunda Uma Devi, Bantu Rajashaker, Nagarapu Lingaiah, Kumar C Ganesh, Pombala Sujitha, Sridhar B
机构信息
Organic Chemistry Division II, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
Organic Chemistry Division II, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India.
出版信息
Eur J Med Chem. 2014 May 22;79:260-5. doi: 10.1016/j.ejmech.2014.04.015. Epub 2014 Apr 5.
A series of novel benzosuberone bearing coumarin moieties 5a-c have been synthesized and their structures were determined by analytical and spectral (FT-IR, (1)H NMR, (13)C NMR, HRMS) studies. The newly synthesized compounds were evaluated for their cytotoxicity against four human cancer cell lines, A549 (Human alveolar adenocarcinoma cell line), HeLa (Human cervical cancer cell line), MDA-MB-231 (Human breast adenocarcinoma cell line), MCF-7 (Human breast adenocarcinoma cell line) and normal cell line HEK293 (Human embryonic kidney cell line). Compound 5a exhibited promising cytotoxicity with IC50 values ranging from 3.35 to 16.79 μM against all the cancer cell lines like A549, HeLa, MCF-7 and MDA-MB-231, while compound 5c showed significant cytotoxicity against HeLa and MDA-MB-231 with IC50 values of 6.72 and 4.87, respectively.
一系列带有香豆素部分的新型苯并环庚酮5a - c已被合成，其结构通过分析和光谱（傅里叶变换红外光谱、氢核磁共振谱、碳 - 13核磁共振谱、高分辨质谱）研究得以确定。对新合成的化合物针对四种人类癌细胞系A549（人肺泡腺癌细胞系）、HeLa（人宫颈癌细胞系）、MDA - MB - 231（人乳腺腺癌细胞系）、MCF - 7（人乳腺腺癌细胞系）以及正常细胞系HEK293（人胚肾细胞系）进行了细胞毒性评估。化合物5a对所有癌细胞系如A549、HeLa、MCF - 7和MDA - MB - 231表现出有前景的细胞毒性，IC50值范围为3.35至16.79 μM，而化合物5c对HeLa和MDA - MB - 231显示出显著的细胞毒性，IC50值分别为6.72和4.87。
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