铁死亡细胞中双光子硫化氢荧光探针的构建与应用

传统的消耗型硫化氢荧光探针因灵敏度较低,无法实现铁死亡过程中细胞内硫化氢含量的检测.基于此,设计并合成了一种双光子激发深红光发射的硫化氢荧光探针KS-HS.探针分子中引入了硫代氨基甲酸苄酯的结构单元,可在碳酸酐酶的催化下释放出H2S从而提高探针的灵敏度.探针分子中的叠氮基与硫化氢发生还原反应,作为触发分子内电荷转移(I...     

Synthesis,Crystal Structure and Antitumor Activity of 4-(5-(2,6-Difluorophenyl)-1,3,4-oxadiazol-2-ylthio)-2-(trifluoromethyl)thieno[2,3-d]pyrimidine

The title compound 4-(5-(2,6-difluorophenyl)-1,3,4-oxadiazol-2-ylthio)-2-(trifluoromethyl)thieno[2,3-d]pyrimidine(C_(15)H_5F_5N_4OS_2, Mr = 416.35) was designed and synthesized as antitumor agent, and its structure was determined by ~1H NMR, ~(13)C NMR, MS, elemental analysis and single-crystal X-ray diffraction. The crystal belongs to monoclinic system, space group P2_1/c with a = 9.904(2), b = 10.057(2), c = 16.595(3) ?, β = 100.000(3)°, V = 1627.9(6) ?~3, Z = 4, F(000) = 832, D_c = 1.699 g/cm~3, μ = 0.395 mm~(-1), R = 0.0468 and wR = 0.1255 for 4726 independent reflections(R_(int) = 0.0336) and 2847 observed ones(I 2σ(I)). The in vitro antitumor activity of the title compound was preliminarily evaluated by the standard MTT assay.     

Synthesis,Crystal Structure and Antitumor Activity of N-(5-Aryl-1,3,4-thiadiazol-2-yl)-N'-((E)-styryl)ureas

N-(5-Aryl-1,3,4-thiadiazol-2-yl)-N?-((E)-styryl)ureas 4 a～4 i were designed and synthesized as antitumor agents, and their structures were characterized by IR, 1 H NMR, 13 C NMR,MS and elemental analysis. The single crystal of compound 4 a, C17 H13 FN4 OS, was also determined by X-ray crystallography. Crystal data: monoclinic, space group P21/n, a = 4.9401(8), b= 8.7100(15), c = 36.604(6) ?, β = 93.320(3)°, V = 1572.4(5) ?3, Z = 4, F(000) = 704, Dc = 1.438 g/cm3, μ = 0.228 mm-1, R = 0.0600 and wR = 0.1448 for 2743 independent reflections(Rint =0.0418) and 2174 observed ones(I 2σ(I)). The in vitro antitumor activities of compounds 4 a～4 i were preliminarily evaluated by the standard MTT assay.