A new Mn(II) complex with the planar ligand 6,7-dicycanodipyrido[2, 2-d: 29, 39-ƒ]quinoxaline (L) [MnL(NO3)(H2O)3]NO 3-CH3OH 3 (1) has been synthesized and characterized by elemental analysis, IR, TG-DTA and molar conductance. Its crystal structure was determined by X-ray diffraction, crystal data: yellow, triclinic, space group P1, Z=2, a =7.3743 (8)Å, b=11.2487 (15)Å, c=14.1655 (15)Å,α=79.412 (2)°,β=83.208(2) °, γ=80.466(2) °. The Mn atom was hexa-coordinated to form a distorted octahedral geometry by two nitrogen atoms of L and four oxygen atoms of three H2O and NO-3 in the complex. The binding mode of the complex with calf thymus DNA has also been investigated with spectrophotometric methods, viscosity and thermal denaturation measurements. The experimental results indicate that the complex intercalated into DNA base pairs via the ligand L. The intrinsic binding constant Kb values for 1 (5.00×10M-1) and L (1.65×105 M-1) were determined by absorption titration and calculated with the model of McGhee and Von Hippel. Biological tests against four different cell lines (HL-60, KB, Hela and BGC-823) in vitro showed that the complex had significant antitumor properties since the 50% inhibition concentrations (IC50) of the complex were within a μM range similar to those of antitumor 50 drug 5-fluorouracil.

蛋白酶体是一种庞大的、多价复合酶，它在承担细胞内蛋白质降解的泛蛋白-蛋白酶体通路（UPP）的关键步骤中起催化作用。UPP不仅可以催化降解异常蛋白质，而且在许多调控蛋白质的更新和加工过程中起重要作用，这些蛋白质的催化过程涉及到人类疾病发病机制的重要生化机制。目前，与UPP有关的酶已被认为是药物设计的分子靶位，蛋白酶体参与调节多种细胞功能，其特异性抑制剂不仅可以作为研究UPP的有利工具，而且也是潜在的抗肿瘤、抗炎药物。本文综述了蛋白酶体抑制剂的药理活性研究进展。