Structure–Function Relationships in Unsymmetrical Zinc Phthalocyanines for Dye‐Sensitized Solar Cells

Let it shine! The impact of the anchoring group on photovoltaic performance by a series of phthalocyanine sensitisers (see figure) has been demonstrated.

     

取代锌酞菁的合成及光物理性质

取代锌酞菁的合成及光物理性质张先付,许慧君（中国科学院感光化学研究所,北京,１００１０１）关键词取代酞菁,合成,光物理性质,电荷转移癌症的光动力疗法及其机制是目前光医学、光生物学及光化学的前沿课题［１］。临床应用的光疗药物──血卟啉有一些难以克服的致...     

Synthesis and Spectroscopic Properties of a Series of New tetra-Substituted Metal Phthalocyanines

A new class of metal phthalocyanines（MPcs） containing four 8-quinolinol（8-QH） derivative moieties were successfully synthesized and characterized by mass spectroscopy, IR, UV-Vis and element analysis, the results of which were consistent with the proposed structures. All of them can dissolve in common organic solvents, such as dichloromethane, chloroform, and acetone. The effect of metal ion on the absorption of Q band was studied with UV-Vis spectra. The fluorescent properties for those complexes were also investigated.     

1-取代苯氧乙酰基-4-芳酰基氨基硫脲的合成及生物活性

苯氧乙酰肼;1-取代苯氧乙酰基-4-芳酰基氨基硫脲的合成及生物活性     

1-取代哌啶-4-酮芳甲酰腙的合成及其抗白血病活性

以取代苄胺或伯胺为原料,依次经过Michael加成、Dieckmann缩合、水解脱羧、酰腙化反应合成了10个未见文献报道的1-取代哌啶-4-酮芳甲酰腙9a～9j,化合物结构经1H NMR,IR,MS和元素分析确证.初步的生物活性测试表明,部分化合物能有效抑制白血病K562细胞的增殖,具有潜在的抗白血病活性.     

1-取代哌啶-4-酮肟醚的合成与杀菌活性测定

以取代苄胺或苯乙胺为起始原料, 依次经Michael 加成, Dieckmann缩合, 水解脱羧, 肟化和醚化等多步反应合成了11个未见文献报道的1-取代哌啶-4-酮肟醚5a～5k. 目标化合物的结构经元素分析, IR, 1H NMR和MS测定确证. 初步杀菌活性测试表明, 部分化合物有较好的杀菌活性.     

2-位或4-位取代吡啶并嘧啶类非经典叶酸拮抗剂的合成及抗肿瘤活性

以非经典叶酸拮抗剂2,4-二氨基-6-(4-甲基苯基)乙基吡啶并[3,2-d]嘧啶(wm-5b)及其侧链简化产物2,4-二氨基吡啶并[3,2-d]嘧啶为先导化合物, 选取具有抗肿瘤活性的基团, 通过微波法高效合成了2-位或4-位取代吡啶并嘧啶类非经典叶酸拮抗剂, 研究了2-位及4-位取代基对抗肿瘤活性的影响, 为非经典叶酸拮抗剂的设计合成提供了更多的理论依据. 目标化合物的结构均经核磁共振波谱(NMR)和质谱(MS)确证. 生物活性测定结果表明, 所有目标化合物均具有抗肿瘤活性, 其中, 6-(4-甲基苯基)乙基-4-氨基-2-(3-氯-4-氟苯基)氨基吡啶并[3,2-d]嘧啶(6b)对HL-60细胞的IC₅₀=(4.09±0.48) μmol/L, 对A549细胞的IC₅₀=(17.99±7.20) μmol/L, 而对HCT116细胞的IC₅₀=(14.52±4.74) μmol/L; 部分目标化合物具有二氢叶酸还原酶抑制活性. 此外, 对部分目标化合物和先导物进行了二氢叶酸还原酶晶体结构的分子对接, 对活性结果和构效关系从分子水平上进行解释.     

酞菁配合物的结构与其光动力抗癌活性

光动力治疗是一种正在发展中的治疗癌症的新方法.主要是利用抗癌光敏剂可优先在 肿瘤组织中富集的特性和随后在适当波长的光照下所引发的光敏化反应来杀死癌肿瘤.自198 5年以来,酞菁配合物作为抗癌光敏剂的研究越来越引人注目. 此文在总结51篇参考文献的 基础上,提出了酞菁配合物的结构与其光动力抗癌活性的某些相关性,着重讨论了中心离子 、环取代基、轴向配体对光动力活性和相关物化性质的影响.得出的一个主要的结论是两亲 性酞菁是极具潜力的光敏剂.     

N-(4-取代苯基-噻唑-2-基)香豆素类亚胺化合物的合成及抑菌活性研究

由含不同取代基的水杨醛与乙酰乙酸乙酯在哌啶存在下反应,得到乙酰基香豆素中间体,再与氨基硫脲缩合,得到含香豆素基的缩氨基硫脲化合物,继而与a-溴代芳基酮发生缩合反应,合成了9个未见报道的新的N-(4-取代苯基-噻唑-2-基)香豆素类亚胺化合物,其结构用IR,1HNMR和HRMS进行了确证,初步生物活性测定实验证明部分目标化合物具有良好的抑菌活性.     

Synthesis of 4-Substituted Bisnaphthalimides

The synthetic route to 4-substituted bisnaphthalimides consisting in reaction of 4-halonaphthalic anhydrides with a,w-diaminoalkanes followed by halogen substitution with dialkylamino group is more promising than imidating coupling of 4-dialkylaminonaphthalic anhydrides for it opens wider synthetic opportunities and ensures better yields of target products. Dihalosubstituted bis-naphthalimides can be prepared by N-alkylation of the corresponding naphthalimides with polymethylene dibromides under conditions of phase-transfer catalysis in the presence of tetraalkylammonium salts.     

以偶氮苯基团为周边取代基的锌酞菁的合成及光物理性质

合成了两种带有偶氮苯周边取代基的锌酞菁化合物,并对其进行了结构表征.与一般酞菁的吸收光谱相比,偶氮苯酞菁的UV-Vis光谱的B带吸收峰强度明显强于Q带.该类化合物在光照条件下表现出重复性较好的顺反异构化性质.Z-扫描结果表明,这类化合物的三阶非线性光学性能主要来源于酞菁的非线性折射率,且β位取代的酞菁的三阶非线性效应大于α位取代的,顺反异构对酞菁的三阶非线性光学性能的影响不大.     

Synthesis and Anti-HIV Activity of a Novel Series of Isoquinoline-Based CXCR4 Antagonists

An expansion of the structure–activity relationship study of CXCR4 antagonists led to the synthesis of a series of isoquinolines, bearing a tetrahydroquinoline or a 3-methylpyridinyl moiety as head group. All compounds were investigated for CXCR4 affinity and antagonism in competition binding and calcium mobilization assays, respectively. In addition, the anti-HIV activity of all analogues was determined. All compounds showed excellent activity, with compound 24c being the most promising one, since it displayed consistently low nanomolar activity in the various assays.     

Synthesis and Biological Activity of α-Substituted 1,2,3-Thiadiazole-4-Acetic Acid Derivatives

Compounds containing 1,2,3-thiodiazole ring were reported to posses fungicidal¹, herbicidal² and growth regulation properties³. For example, N-phenyl-N'-1,2,3-thiadizazol-5-yl-urea (Thidiazuron, Dropp) has been used as a cotton defoliant⁴, herbicide and was also found to exhibit cytokinin-like activity in bioassay systems. The compound was more effective than Zeatin⁵ and 6-BA⁶. Because the synthesis of 1,2,3-thiodiazole ring is difficult,compounds containing 1,2,3-thiadiazole ring are relatively seldom reported. Herein, we report the synthesis of a novel series of α-substituted-1,2,3-thiadiazole-4-acetic acid derivatives.     

8-取代黄酮的合成及生理活性研究

设计合成了8-黄酮甲基氮芥和6种8-黄酮甲基多聚异戊二烯胺类化合物, 产物结构经¹H NMR, MS及元素分析确证. 合成的7个化合物与氮芥类抗肿瘤药物美法仑一起对白血病细胞(K562)、中国仓鼠卵巢细胞(CHO)、黑色素瘤细胞(B16)等3种肿瘤细胞进行了初步的体外生理活性测试. 结果表明, 对3种受测细胞, 8-黄酮甲基氮芥的体外活性均与美法仑接近; N,N-二(8-黄酮甲基)香叶基胺则表现出比美法仑更高的体外抗肿瘤活性.     

Synthesis and Cytotoxic Activity of 4-Substituted 3-Cyano-6,6-dimethyl-5,6-dihydro-2-pyranones

The respective 4-(arylvinyl)lactones and compounds of the Michael adduct type were synthesized by the condensation of substituted benzaldehydes with 3-cyano-4,6,6-trimethyl-5,6-dihydro-2-pyranone in the presence of catalytic amounts of sodium hydroxide. It was shown by the semiempirical AM1 method that the indicated products can be formed through one and the same intermediate compound. Some of the synthesized phenylvinyl-5,6-dihydro-2-pyranones have a cytotoxic effect, and this corresponds to the prognosis of the OREX expert system.     

无溶剂研磨法合成3-取代色满-4-酮衍生物及其抑菌活性研究

以6-卤代或未取代色满-4-酮为原料,在碱催化的条件下采用无溶剂研磨法与醛发生缩合反应,合成一系列新型的3-取代色满-4-酮衍生物3a~3t,并通过IR、1H NMR、13C NMR、HRMS对所合成的化合物进行结构表征。抑菌活性测试结果表明,所合成的化合物对大肠杆菌、枯草杆菌、金黄色葡萄球菌均有不同程度的抑菌活性。     

新型4-取代四氢咪唑烷的合成

以三氟醋酸催化N-甲氧基-N-_甲硅甲基苄胺生成非稳定型亚甲胺基叶立德;再与N-Ts醛亚胺完成1,3-偶极环加成反应合成了10个新的4-取代四氢咪唑烷,收率80%-99%,其结构经1H NMR和13C NMR表征.     

3-(2-取代噻唑-4-基)愈创兰烃薁的合成及抗菌活性

以3-氯乙酰基愈创兰烃薁、硫脲或硫代酰胺为原料, 一锅法合成了一系列3-(2-取代噻唑-4-基)愈创兰烃薁衍生物. 该反应收率良好、操作简单、条件温和. 产物的结构通过红外光谱、核磁共振谱和元素分析证实. 对所合成化合物进行了抗菌活性测试, 初步表明具有活性.