卟啉衍生物作为G-四链体DNA结合剂的研究进展

综述了卟啉衍生物作为G-四链体DNA结合剂的研究进展,其中涉及该类化合物作为G-四链体DNA结合剂的设计合成、亲和能力以及端粒酶抑制活性.     

新型萘酰亚胺衍生物的合成

N-(N’,N’-二甲基氨基乙基)-4-硝基-1,8-萘酰亚胺和2,3-二甲基苯并噻唑碘化盐在痕量水存在下经亲核取代反应合成了一个新型的萘酰亚胺衍生物——N-(N’,N’-二甲基氨基乙基)-4-[2-(2,3-二氢-2,3-二甲基苯并噻唑)氧基]-1,8-萘酰亚胺,其结构经1H NMR,13C NMR和ESI-MS表征。并对反应机理进行了初步研究。     

新型树枝功能化萘酰亚胺类发光材料的合成及其光放大效应

在树枝(dendron)上引入特定的功能单元,将多个具有特定功能团(咔唑)连接起来．形成功能化树枝状周边分子团簇,然后将它们分别与核心色素萘酰亚胺相连接,合成新型周边树枝状功能化的有机发光材料(共三代)。稳态荧光研究发现周边功能团吸收的能量能以较高的效率传递给中心核色素萘酰亚胺。其传输效率与化合物的树枝代数密切相关,具有特殊的光采集、光放大效应。瞬态荧光研究表明树枝化合物中的咔唑单元都呈双指数衰减特征,其中较短荧光寿命成分是咔唑和萘酰亚胺单元之间的相互作用。     

Rational Design of Star-shaped Molecules with Benzene Core and Naphthalimide Derivatives End Groups as Organic Light-emitting Materials

A series of star-shaped molecules with benzene core and naphthalimides derivatives end groups have been designed to explore their optical,electronic,and charge transport properties as charge transport and/or luminescent materials for organic light-emitting diodes(OLEDs). The frontier molecular orbitals(FMOs) analysis has turned out that the vertical electronic transitions of absorption and emission are characterized as intramolecular charge transfer(ICT). The calculated results show that the optical and electronic properties of star-shaped molecules are affected by the substituent groups in N-position of 1,8-naphthalimide ring. Our results suggest that star-shaped molecules with n-butyl(1),benzene(2),thiophene(3),thiophene S?,S?-dioxide(4),benzo[c][1,2,5]thiadiazole(5),and 2,7a-dihydrobenzo[d]thiazole(6) fragments are expected to be promising candidates for luminescent and electron transport materials for OLEDs. This study should be helpful in further theoretical investigations on such kind of systems and also to the experimental study for charge transport and/or luminescent materials for OLEDs.     

ESI Mass Spectrometric Exploration of Selective Recognition of G-Quadruplex in c-myb Oncogene Promoter Using a Novel Flexible Cyclic Polyamide

In this research, electrospray ionization mass spectrometry (ESI-MS) was used to probe the binding selectivity of a flexible cyclic polyamide (cβ) to G-quadruplexes from the long G-rich sequences in the c-myb oncogene promoter. The results show that three G-rich sequences, including d[(GGA)₃GGTCAC(GGA)₄], d[(GGA)₄GAA(GGA)₄], and d[(GGA)₃GGTCAC(GGA)₄GAA(GGA)₄] species in the c-myb promoter can form parallel G-quadruplexes, and cβ selectively binds towards these G-quadruplexes over both several other G-quadruplexes and the duplex DNA. These properties of cβ have profound implications on future studies of the regulation of c-myb oncogene expression.

Synthesis of Novel Benzisothiazolone Derivatives as Potential Antifoulants

Novel antifoulant 2‐(3‐oxobenzo[d]isothiazol‐2(3H)‐yl)acetohydrazide (2) and 3‐oxobenzo[d]isothiazol‐2(3H)‐yl acetic acid [1‐phenylmethylidene]‐hydrazides (3a–3h) were synthesized in good yields, and their structures were characterized by means of UV, IR, ¹H NMR, MS, and elemental analysis.     

二苯乙炔类MRI分子探针的合成

以4-取代苯乙酮为起始原料,经过Vilsmeier反应和Sonogashira偶联反应合成了可用作潜在阿尔茨海默病MRI分子探针的2-(2-氟-5-吡啶基)取代苯乙炔(1a～1c)和2-对氟苯基(取代)苯乙炔(1d～1f),其结构经1HNMR,13CNMR和IR表征。其中1a～1c和1f未见文献报导。     

Synthesis of Novel Quinazoline Derivatives as Antimicrobial Agents

Quinazoline isothiocyanate 1 reacts with various nucleophiles(nitrogen nucleophiles,oxygen nucleophiles and sulphur nucleophiles)to afford heterocyclic systemes 2-13,Also,the [4 2] cycloaddition reaction of 1 with phenyl isocyanate,benzylidene aryl amine and cinnamic acid derivatives gave novel heterocyclic compounds 14-16,Moreover,the reaction of 1 with active methylene compounds under Michael reaction conditions also was investigated to yield 17 and 18 and it was found that all these reactions proceede via isothiocyanate heterocyclization to furnish non-condensed heterocyclic compoundes,Some of the newly synthesized compounds were tested for their antimicrobial activities.     

Synthesis and Evaluation of Two Novel Naphthol Derivatives as Novel Cholinesterase Inhibitors

Two novel naphthol derivatives(1 and 2) were synthesized and characterized via IR,~1H NMR,and HRMS.The structure of compound 2 was verified by single-crystal X-ray crystallography.It crystallizes in monoclinic,space group C2/c with a = 21.6725(9),b = 6.0127(3),c = 25.5405(14) ?,β = 94.716(5)o,V = 3316.9(3) ?~3,Z = 8,F(000) = 1384,D_c = 1.511 Mg/m~3,M_r = 377.22 and μ = 2.487 mm~(-1).In addition,their cholinesterase inhibitory activities in vitro toward Electrophorus electricus acetylcholinesterase(eel ACh E) and horse serum butyrylcholinesterase(eq BCh E) were further determined.The results showed that compound 1 as a new acetylcholinesterase(ACh E) inhibitor displayed higher ACh E inhibitory activity(IC_(50) = 1.4 μM),which could be considered for Alzheimer's disease therapeutics.     

Investigation of H-Complex Formation of Derivatives of Naphthalimide with Phenol by IR Spectroscopy

The H-complex-forming reaction of naphthalimide derivatives with phenol has been investigated by IR spectroscopy. It was shown that for the majority of compounds studied the carbonyl group is the main center of basicity. In the case of amino-substituted imides of naphthalic acid transfer is possible of the reaction center from the carbonyl group to the nitrogen atom of the substituent introduced into the naphthalene ring. However because of steric hindrance this occurs only for amino- and methylamino-substituted naphthalimide.     

Selective Halogenation of L-Sorbose Derivatives

Abstract

Deoxyhalogenosugars constitute an important class of compounds for the synthesis of other carbohydrate derivatives.^1–3 Several members of this class are of interest in their own right, being intensely sweet^{4, 5} or possessing anti-cariogenic^6,7 or male anti-fertility properties.^8–11     

新型吲哚抗癌试剂的设计与合成

以邻碘苯胺和苯乙炔为原料,经10步反应合成了2,3-二取代的新型吲哚抗癌试剂,总收率33%~37%,其结构经1H NMR和MS表征。     

Selective Reduction of gem-Dichlorocyclopropane Derivatives

Cyclopropane derivatives frequently occur as subunits of some natural products as wellas intermediates of medicines and pesticides'. We are interested in the synthesis of I chloro-2,2,3,3-tetramethylcyclop during our synthesis of some new compounds inasymmetric catalysis and in combinatorial chemistry. Closs has synthesized thiscompound via the addition of manochlorocarbene to alkene2. Safiev obtained it via theaddition of monochlorocarbene in PTC-supersonic conditions3. More recently,Bagdan…     

Synthesis of Novel Ligustrazine Derivatives as Potential Platelet Aggregation Inhibitors

Ligustrazine (lig; tetramethylpyrazine, TMP; Figure 1) is one of major efficient components from Chinese traditional medicine herb Ligusticum Chuanxiong Hort, which is currently widely used in China for the treatment of coronary atherosclerotic cardiovasc…     

Microwave-Assisted Synthesis of Some Novel 1,2,3,4-Tetrahydropyrimidine Derivatives as Antidiabetic Agents

Russian Journal of Organic Chemistry - An efficient and rapid microwave irradiation protocol have been developed for the synthesis of a new series of...     

Selective Synthesis Substituted Derivatives of Hexa-peri-hexabenzocoronenes

Polycyclic aromatic hydrocarbons have been intensively studied in recent years. [1,2] They consist of flat disctype cores surrounded by flexible chains, which enable them to self-assemble into columnar mesophases. The packing behavior of these discotic liquid crystals renders them well suited materials for the study of one-dimensional transport processes such as electrical conductivity and photoconductivity along the columnar axis. These compounds also have good fluorescent property. We would like to report the design and synthesis of mono- or multi-substituted hexa-peri-hexabenzocoronenes and study the fluorescent property and structure relationship.     

Synthesis of Novel Maleonitrile Derivatives

The synthesis of four novel maleonitrile derivatives are described. New maleonitriles have been prepared by the reaction of different alkylhalides such as 3-bromopropionitrile, 1,3-dichloroacetone, α, α′-dibromoxylene, and p-nitrobenzylbromide with dithiomaleonitrile disodium salt. All novel compounds have cis-cyano groups and are characterized by IR, NMR spectroscopy, and elemental analysis.