吩噻嗪衍生物的合成及其光敏抗肿瘤作用研究

Synthesis and photosensitive antitumor effect of phenothiazine derivatives

为了发现更为有效的光敏药物,以吩噻嗪为母体,设计合成4个吩噻嗪衍生物(C1~C4),采用^(1)HNMR和MS对其结构进行了表征。紫外-可见吸收光谱显示其最长吸收波长约为670 nm;荧光发射光谱表明其最大发射波长约为713 nm;MTT法表明这些化合物对ECA-109均有显著的光动力抑制作用。其中化合物C2和化合物C3在浓度为6μmol/L用650 nm激光照射(4 J/cm^(2))时,对ECA-109抑制率分别高达85%和84%,光动力抗肿瘤作用明显,值得进一步研究开发。

To find more effective photodynamic drug.Four phenothiazine hydrochloride derivatives(C1~C4)were designed and synthesized,and their structures were characterized with ^(1)H NMR and MS.These compounds have obvious absorption at about 670 nm in the ultraviolet-visible absorption spectrum,and emission at about 713 nm in the fluorescence emission spectrum.Among them,compounds C2 and C3 had outstanding photodynamic anti-tumor effects with inhibitory rates 85% and 84% respectively at concentration 6 μmol/L under 650 nm laser irradiation(4 J/cm^(2)),which deserves further investigation as potential photosensitive drugs in PDT.