Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), SAS Nagar, Punjab, India.
Bioorg Med Chem Lett. 2012 Mar 15;22(6):2251-6. doi: 10.1016/j.bmcl.2012.01.089. Epub 2012 Jan 31.
A series of dimeric phloroglucinol compounds were synthesized in a single step using commercially available phloroglucinol and methanesulfonic acid. Based on the reported anticancer activity of plant derived dimeric phloroglucinols, these synthesized compounds were evaluated for their in vitro anti-proliferative activities against various cancer cell lines. Several compounds demonstrated in vitro cytotoxic effects across a wide array of tumor cell types. The compound 29 with pyridin-3-yl group on linker methylene and two diisovaleryl phloroglucinol moieties was found to be the most active in all the five cancer cell lines having a low IC(50) of 5.5 μM in colon cancer cell lines (HCT116).
使用商业上可获得的间苯三酚和甲磺酸，以一步法合成了一系列二聚间苯三酚化合物。基于植物来源的二聚间苯三酚的报道的抗癌活性，对这些合成的化合物进行了体外抗增殖活性评估，以对抗各种癌细胞系。几种化合物在广泛的肿瘤细胞类型中表现出体外细胞毒性作用。带有吡啶-3-基的连接亚甲基和两个二异戊酰基间苯三酚部分的化合物 29 在所有五种癌细胞系中最为活跃，在结肠癌细胞系（HCT116）中的 IC50 低至 5.5 μM。
