Pharmaceutical Research Center, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, China.
Bioorg Med Chem Lett. 2013 Mar 1;23(5):1297-301. doi: 10.1016/j.bmcl.2012.12.098. Epub 2013 Jan 9.
A series of dimethylaminomethyl-substituted curcumin derivatives/analogues were designed and synthesized. All compounds effectively inhibited HepG2, SGC-7901, A549 and HCT-116 tumor cell lines proliferation in MTT assay. Particularly, compounds 2a and 3d showed much better activity than curcumin against all of the four tumor cell lines. Antioxidant test revealed that these compounds had higher free radical scavenging activity than curcumin towards both DPPH and galvinoxyl radicals. Furthermore, the aqueous solubility and stability of the target compounds were also significantly improved compared with curcumin.
设计并合成了一系列二甲氨基甲基取代的姜黄素衍生物/类似物。所有化合物在 MTT 测定中均有效抑制 HepG2、SGC-7901、A549 和 HCT-116 肿瘤细胞系的增殖。特别是化合物 2a 和 3d 对所有四种肿瘤细胞系的活性均优于姜黄素。抗氧化试验表明，与姜黄素相比，这些化合物对 DPPH 和半胱氨酸自由基具有更高的自由基清除活性。此外，与姜黄素相比，目标化合物的水溶解度和稳定性也得到了显著提高。
