175 results about "Naphthalimides" patented technology

The invention relates to bis 1,8 naphthalimide compounds including antibody drug conjugate (ADC) compounds represented by Formula I: Ab-(L-D)p   I where one or more 1,8 bis-naphthalimide drug moieties (D) having Formulas IIa and IIb are covalently linked, through the wavy line, by a linker (L) to an antibody (Ab). The invention also relates to heterocyclic-substituted 1,8 bis-naphthalimide compounds having Formula XV The invention also relates to pharmaceutical compositions comprising an effective amount of a Formula I ADC or Formula XV heterocyclic-substituted 1,8 bis-naphthalimide compound for treatment of hyperproliferative disorders and other disorders. The invention also relates to methods for killing or inhibiting the proliferation of tumor cells or cancer cells including administering to a patient an effective amount of a Formula I ADC or Formula XV compound.

Bis 1,8 naphthalimide compounds including antibody drug conjugate (ADC) are described. Pharmaceutical compositions comprising an effective amount of a 1,8 bis-naphthalimide compound for treatment of hyperproliferative disorders and other disorders are described. Methods are described for killing or inhibiting the proliferation of tumor cells or cancer cells including administering to a patient an effective amount of a 1,8 bis-naphthalimide compound.

The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to naphthalimides such as amonafide or analogs, derivatives, or prodrugs thereof.

The invention relates to a pillar[5]arene / isophthalic acid-1,8-naphthalenedicarboximide complex. The complex uses copillar[5]arene as a subject, isophthalic acid-1,8-naphthalenedicarboximide as an object and C-H...PI and electrostatic force as driving force; and a part of isophthalic acid-1,8-naphthalenedicarboximide with negative charges is included into the cavity of copillar[5]arene through self-assembling in an alkaline environment, so the process of assembling of the subject and the object is finished. After aluminum ions are added into a solution of the pillar[5]arene / isophthalic acid-1,8-naphthalenedicarboximide complex, the fluorescence of the complex solution is enhanced and yellow fluorescent light is given out; and when anionic CN<-> is further added, the fluorescence of the complex solution undergoes a red shift and green fluorescent light is given out. Therefore, the pillar[5]arene / isophthalic acid-1,8-naphthalenedicarboximide complex is applicable as a novel supramolecular fluorescence sensor for continuous detection of Al<3+> and CN<-> in environment.

The invention designs and synthetizes a supermolecule polymer framework material. The supermolecule polymer framework material is formed through self assembly in cyclohexanol by using naphthalimide functionalized pillar [5] arene as a subject and bilateral quaternization pillar [5] arene as an object, wherein the mole ratio of the subject to the object is 1:1. Through competitive coordination mechanism, the supermolecule polymer framework material (SOF-AP5-MJP5) and a metal supermolecule polymer framework material (M-SOF-AP5-MJP5) can respectively realize continuous response and high-sensitivity detection to Fe<3+> and H2PO4<->; the recognition performance has important application values in the field of ion recognition.

The invention discloses a fluorescence probe for detecting glutathione and a preparation method and a use method of the fluorescence probe. A classical ICT system is constructed by utilizing 1,8-naphthalimides, a benzene sulfoxide part is introduced at 4-position, and the ICT effect of probe molecules is adjusted and controlled by utilizing a classical ICT system constructed by 1,8-naphthalimide and introducing benzene sulfoxide part at the fourth position. Under the condition that no glutathione exists, the probe molecules do not emit fluorescence light because of strong electron-withdrawing effect of 4-position benzene sulfoxide; under the condition that glutathione exists, the benzene sulfoxide part can be replaced by the glutathione, and thus intramolecular electron transfers from a 4-position sulphur atom (from the glutathione) to the 1,8-naphthalimides, and the probe molecules emit hyperfluorescence because of the ICT effect. According to the invention, the detection of the intracellular glutathione can be realized, and the fluorescence probe has the advantages of convenient operation, low cost, sensitive response, easy promotion and application and the like.

The invention provides a fluorescent probe for detecting formaldehyde in cell endoplasmic reticulums. The chemical name of the fluorescent probe is 4-hydrazino-N-(2-aminoethyl-4-methyl benzenesulfonamido)naphthalimides, and the short name is Na-FA-ER. The invention further discloses properties and functions of the probe in the fields of fluorescence detection and bioimaging. According to the fluorescent probe, the fluorescence intensity of a probe solution is gradually strengthened along with the increase of formaldehyde concentration, so that the probe has relatively good application values in sensing detection of formaldehyde in in-vivo and in-vitro environments and has certain contribution for prevention and control work of formaldehyde.

The invention discloses gelators PC5 based on naphthalimide functionalized pillar[5]arene. Organic supramolecular gel PC5G with yellow aggregate state induced fluorescence can be formed by the gelators in a cyclohexanol solution under the external-wall pi-pi action. When Fe<3+> is added to PC5G, Fe<3+> can produce cation-pi action with naphthalimide, and the external-wall pi-pi action between thegelators is damaged, as a result, fluorescence of PC5G is quenched; when H2PO4<-> is added to metallogel PC5-FeG after fluorescence quenching, H2PO4<-> and Fe<3+> are complexed, the external-wall pi-pi action of PC5G is restored again, and aggregate state induced fluorescence appears again, so that continuous reversible supersensitive detection for Fe<3+> and H2PO4<-> is realized. Besides, the organic supramolecular gel PC5G can remove Fe<3+> from an aqueous solution very well, and removal rate is up to 99.42%.

The invention provides a 1,8-naphthalimide-based light-controlled fluorescent molecular switch compound bonded with a bis-spilenpyran unit and a synthesis method and application of the compound. Firstly, bis-spiropyran is modified to a 1,8-naphthylimide molecule through a covalent bond, the compound shows a good photochromic effect and light-controlled two-color fluorescent molecular switch performance in an organic solvent and a solid medium, the fluorescence resonance energy transfer efficiency of the compound is greatly improved, and the thermodynamic stability and photosensitivity of the compound are also high. The 1,8-naphthalimide-based light-controlled fluorescent molecular switch compound bonded with the bis-spilenpyran unit and the synthesis method and application of the compoundcan be used in the field of ion detection and photochemical imaging of biological systems.

A phosphino-based mapropyl copolymer containing fluorescent group and its production are disclosed. The process is carried out by taking 4-bromine-1,8-naphthalic anhydride, glacial acetic acid and N, N-dimethyl-ethylenediamine as raw materials to obtain 4-bromine-N-(2-N,, N,-dimethylbenzidine-ethyl)naphthalimide, reacting it with sodium methoxide to induce methoxy-group to obtain 4-methoxy-N-(2-N,, N,- dimethylbenzidine-ethyl)naphthalimide, reacting it with allyl chloride to obtain fluorescent monomer 4-methoxy-N-(2-N,, N,- dimethylbenzidine-ethyl)naphthalimide allyl ammonia chloride with fluorescent characteristic and double-bond, polymerizing it with sub-sodium phosphate, maleic anhydride, acroleic acid and propenyl-sodium sulfate to obtain the final product. It has fluorescent tracting, corrosion-inhibting, scale-inhibiting and dispersion functions.

The invention provides a specific fluorescence probe substrates of human carboxylesterase 2 (CES2) and application thereof. The specific probe substrate is a benzoateb compound of a C4 hydroxyl naphthalimide, and is applicable to determine the enzyme activity of CES2 in a biological system. The CES2 enzyme activity determination flow comprises: selecting a hydrolysis benzoyl-removal reaction of the benzoate compound of the C4 hydroxyl naphthalimide as a probe reaction, and quantitatively determining the generation amount of a hydrolysis metabolite of the compound in a unit time, so as to determine the enzyme activity of CES2 in all biological samples, cells, bodies and integral organs. The probe is applicable to quantitative assessment of CES2 enzyme activity in biological samples of different species and different individual sources, and quantitative determination on CES2 enzyme activity in different sources of animal tissue cell culture fluids and cell preparation substances, so that the probe is expected to help to realize assessment on medicine disposal capability of important drug metablic enzyme CES2. Additionally, the probe also is applicable as an inhibitor for rapidly screening CES2 in vitro by means of the probe reaction.

The invention relates to a designed synthesized gel factor capable of recognizing an aromatic acid isomer. Acetonitrile is taken as a solvent and brominated column [5] aromatic hydrocarbon and a naphthalimide derivative are taken as a substrate to carry out reflux, after the reaction is over, the reaction system is cooled to the room temperature, the solvent is steamed, and petroleum ether and ethyl acetate are used for elution to obtain a yellow solid product which is the gel factor BP5. The gel factor BP5 can form supramolecular polymer gel BP5G in cyclohexanol through a pi-pi effect. The supramolecular gel BP5G allows color comparison and fluorescent recognition and separation of aromatic acid isomer molecules to be achieved through competitive coordination of hydrogen bonds. Multifunction application including recognition and separation of the aromatic acid isomer is achieved, and the gel factor has great significance in the fields of bioscience and environmental detection.

The invention discloses fluorescent test paper capable of rapidly detecting formaldehyde. The fluorescent test paper is formed by fluorescent-whitening-agent-free test paper loaded with fluorescent probe naphthalimides derivative. The fluorescent test paper is deep green, the size of the test paper is (100-75)mm*(15-8)mm*(1-0.5)mm, the content of the naphthalimides derivative loaded on each fluorescent test paper is not less than 0.01mg, the test paper for a substrate is deep-green precision pH test paper, and the naphthalimides derivative loaded on the test paper for the substrate is N-amino-4-(1-piperazinyl)-1,8-naphthalimide, N-amino-4-(1-piperazinyl)-1,8-naphthalimid or N-amino-4-(1-pyrrolidinyl)-1,8-naphthalimide. The fluorescent test paper is easy to prepare, convenient to use and capable of rapidly and accurately detecting and determining the formaldehyde in the environment.

The invention belongs to the technical field of fluorescence detection materials and discloses an enhanced fluorescent probe and a preparation method and application thereof. The fluorescent probe is 5-{4-[3-(2-{2-[2-(toluene-4-sulfamine)-ethyl]-1H-benzo(de)isoquinoline-1,3(2 H)-diketone-6-amino}-ethylamino)-propoxy]-phenylazo}-2-hydroxybenzoic acid and has a molecular structural formula shown in a formula (1). The probe compound is prepared from visible light excited and emitted fluorescent chromophore naphthalimides and an azo reductase recognition group 5-aminosalicylic acid azobenzene derivative. The probe compound not only has better water solubility, but also is high in accuracy when being used for azo reductase detection, is convenient to use and can simultaneously trace release of anti-inflammatory drugs such as 5-aminosalicylic acid and provide a supplementary means for diagnosis and treatment of colitis.

The invention discloses an ultramolecular gelator MP5 based on naphthalimide functional column 5 arene. The gelator can form organic ultramolecular gel MP5-G with yellow aggregation induced fluorescence in a cyclohexanol solution under the action of pi-pi; the organic ultramolecular gel can be used for detecting Fe<3+> with high selectivity and super sensitivity: when ions such as Fe<3+>, Hg<2+>,Ag<+>, Ca<2+>, Cu<2+>, Co<2+>, Ni<2+>, Cd<2+>, Pb<2+>, Zn<2+>, Cr<3+> and Mg<2+> are added into the MP5-G, fluorescence is quenched only by the Fe<3+>, and stable metal gel MP5-FeG is formed. When L-Cys is added into the fluorescence-quenched metal gel, the L-Cys and the Fe<3+> are complexed to recover the pi-pi action again among the MP5-G, so that aggregation induced fluorescence appears again,and continuous reversible ultrasensitive detection of the Fe<3+> and the L-Cys is realized.

The invention provides a fluorescent probe Na-FA-Mito. The fluorescent probe has the advantages that the reaction is sensitive, the detection limit is low, and the specificity is good; the fluorescentprobe can be used for detecting formaldehyde-targeted mitochondria. The chemical name of the fluorescent probe is brominated N-(2-formamido ethyl-N-(3-triphenyl phosphine propyl))-4-hydrazino-1,8-naphthalimide salt. The fluorescent probe is used for detecting the formaldehyde in solutions or cells.

The invention relates to the use of 1,8-naphthalimide derivatives and of their salts as scintillation agents and more specifically as agents for discriminating between fast neutrons and gamma rays.It also relates to liquid scintillators comprising these scintillation agents in solution in a solvent and to novel 1,8-naphthalimide derivates of use as scintillation agents, in particular for discriminating between fast neutrons and gamma rays.Applications: all the fields of use of scintillators and in particular industry, geophysics, fundamental physics, in particular nuclear physics, the safety of goods and people, protection from radiation of workers in the industrial, nuclear and medical sectors, medical imaging, and the like.

The invention discloses a fluorescence probe for detecting hydrogen sulfide as well as a preparation method and application method of the fluorescence probe. A classic ICT system is constructed by 4-oxhydryl-1,8-naphthalimides; an azide benzyl part is directly introducd at 4-bite, so that the ICT system has biological and optical stability. An azide group is restored into amino by the hydrogen sulfide in presence of the hydrogen sulfide, so that a 4-toluidine part is separated by 1,6-removal, so as to obtain the 4-oxhydryl-1,8-naphthalimides. A 'ratio meter' type hydrogen sulfide probe of naphthalimides dyes and a special detection kit for the hydrogen sulfide probe have good response to a hydrogen sulfide solution; detection of hydrogen sulfide in a cell can be achieved; and the fluorescence probe has the advantages of being simple and convenient to operate, low in cost, sensitive in response, easy to popularize and apply and the like.

The invention discloses water-dispersible multicolour fluorescent polymer nanoparticles and a preparation method thereof. The water-dispersible multicolour fluorescent polymer nanoparticles are prepared by taking methyl methacrylate as a monomer, taking 4-ethyoxyl-9-allyl-1,8-naphthalimide (EANI), 4-amido-7-nitro-N-allylbenzo[1,2,5] oxadiazole (NBDAA), and Nile red methacrylate (NRME) as polymerizable fluorescent dyes, taking lauryl sodium sulphate (SDS) as a surfactant, and using a one-step miniemulsion polymerization method. The water-dispersible multicolour fluorescent polymer nanoparticles are great in dispersibility in water, quite high in fluorescent brightness, and capable of emitting multicolour fluorescence from blue to red under the excitation of a single wave. The water-dispersible multicolour fluorescent polymer nanoparticles obtained by the preparation method disclosed by the invention are uniform in size, and good in structure and light stability, has a fluorescence emission signal capable of being adjusted for many times in a wide interval under a single excitation wavelength, is simple in synthesis route, convenient to use, suitable for amplification synthesis and actual production applications, and has a great application prospect in the fields of biological encoding and multiple biological analysis.

Novel substituted naphthalimide derivatives of formula (I) and (II), pharmaceutically acceptable salts thereof and solvates thereof, are useful for making pharmaceutical compositions for the treatment of cell proliferative diseases such as cancer. The invention also provides methods for making such derivatives.

The invention discloses a new compound in henbane and a preparation method and application thereof, and belongs to the field of the extraction method for Chinese traditional medicaments. A method for extracting the compound grossamide comprises the following steps: extracting 6-methoxy-7-hydroxy-1-(3-methoxy-4-hydroxyphenyl)-2-[(4-hydroxyphenyl)-ethyl]-2,3- naphthalimide. The preparation method comprises the following steps: extracting henbane seed by reflux of ethanol to obtain henbane total extract, dissolving and dispersing the total extract with distilled water at firstly, then extracting the obtained product with petroleum ether and ethyl acetate to obtain ethyl acetate extract, and obtaining a compound henbane amide from the ethyl acetate extract by silica gel column chromatography and preparative liquid chromatography. The compound has a certain inhibition effect on the growth of breast cancer cells and leukemia and tumor cell, and shows the application prospect as a novel antitumor medicament.

The invention discloses a low-toxicity 1,8-naphthalimide derivative and a synthetic method and application thereof. The synthetic method of the 1,8-naphthalimide derivative mainly comprises the following steps: dissolving amonafide and 2-fluorobenzoyl chloride in an organic solvent and reacting; and after reaction is finished, removing a solvent to obtain a coarse product as a target object. Testsshow that the derivative has remarkable bioactivity, and particularly has remarkable inhibition activity to non-small cell lung cancer cell strains HCC-827 and other tumor cell strains, moreover, toxic and side effects of human normal cells are small, and thus, the 1,8-naphthalimide derivative is expected to be developed into a targeted therapy drug. The structure of the 1,8-naphthalimide derivative is as shown in a formula (I) as shown in the specification.

The invention discloses a 1,8-naphthalimide derivative as well as a synthesis method and an application thereof. The derivative is N-(3,4-methylene dioxophenethyl)-4-(3-N,N-dimethylamino)propylamino-1,8-naphthalimide; and the compound is prepared by taking 4-bromo-1,8-naphthalic anhydride as a raw material which sequentially reacts with 3,4-methylene dioxophenylethylamine and N,N-dimethyl-1,3-diaminopropane. The synthesis method is simple and easy to control. The applicant observes the proliferation inhibition activity of the 1,8-naphthalimide derivative on 9 human tumor cell strains and two normal cell strains, and the results indicate that the in-vitro antitumor activity is remarkable and the 1,8-naphthalimide derivative has relatively good potential medicinal value and is expected to be applied to the preparation of various anti-tumor drugs. The chemical structural formula of the compound disclosed by the invention is shown by the formula (I).

The invention discloses a ratio type fluorescent probe substrate for cytochrome oxidase CYP1A and an application thereof. The specific probe substrate has a hydroxynaphthalimide alkane acid structure and can be used for determining the CYP1A enzymatic activity in a biosystem. A flow for determining the CYP1A enzymatic activity comprises the following steps: selecting a hydroxynaphthalimide alkane acid demethylation reaction as a probe reaction, and determining the CYP1A enzymatic activity in various biological samples by quantitatively detecting the production amount of demethylation metabolites in a unit time. The ratio type fluorescent probe substrate disclosed by the invention can be used for quantitative evaluation for the CYP1A enzymatic activity in biological samples of different species and different individual sources and for quantitative determination for the CYP1A enzymatic activity in different-source animal tissue cell culture fluids and cell prepared products, so as to realize evaluation for the medicine disposition capacity of the important medicine metabolizing enzyme CYP1A. In addition, the probe reaction can also be used for rapidly screening a CYP1A inhibitor in vitro and evaluating the inhibition capacity of the inhibitor.

Record material imageable with a laser beam. The material is a substrate such as paper or polyolefin film having provided on at least one surface thereof a coating containing a solvent-soluble or disperse-type dye suitable for coloring plastics or polymers. Typical solvent-soluble and disperse-type dye include monoazo dyes, diazo dyes, anthraquinone dyes, coumarin dyes, quinoline dyes, xanthene dyes, and naphthalimide dyes. The record material does not show visible dye specks in the coating layer on the substrate because the dye has a very small average particle size—less than 50 microns. No more than 1% of the dye particles are larger than 100 microns. Also, method for imaging a substrate using heat energy by applying heat energy to the described record material to bring about a temperature in the coating greater than the melting temperature of the dye, causing color to become visible in the record material.

The invention relates to a film with room temperature phosphorescence and a preparation method thereof. The method is mainly characterized in that alkyl halogenated amine salt containing naphthalimides is doped into benzene alkyl halogenated amine salt; self assembly is performed with lead halide in organic solvents; next, film forming is performed by a solution method. The obtained organic and inorganic hybrid perovskite film containing naphthalimides has the monomolecular room temperature phosphorescence; in addition, the phosphorescence quantum yield is high; the rotary coating film formingcan be realized. By changing the types of the perovskite halogen atoms, the luminescence of the film can also be regulated to become from the emission of single phosphorescence into the simultaneousemission of fluorescence and phosphorescence. The perovskite film material also has the advantages that the preparation method is simple; the synthesis temperature is low; the stability is high, and the like. The material is suitable for industrial production, has practicability and has wide application prospects in the fields of safe ink, anti-counterfeiting recognition and the like.

The invention discloses a fluorescence probe used for malonaldehyde imaging inside living cells and a preparation method thereof and belongs to the technical field of biological fluorescence analysis. The fluorescence probe is obtained in the following way: benzoyl hydrazine (containing substituted benzoyl hydrazine) as the effective part of the probe and malonaldehyde and 1,8-naphthalimide as a fluorescence reporter group are connected through a certain linking group (such as imino group). The fluorescence probe can effectively detect malonaldehyde in a physiological environment, and endogenous and exogenous malonaldehyde bioimaging in living cells is successfully realized. Malonaldehyde bioimaging in living cells is realized for the first time in the invention. The optimal probe MDAP-1 has high sensitivity (the lowest detection limit reaches 0.6micron), strong fluorescence response and short response time, has excellent selectivity to malonaldehyde, but has no fluorescence response to metal ions, oxidation active products and active carbonyl compounds, etc.

Disclosed are a 1,8-naphthalimide derivative, a preparation method therefor and a use thereof. The 1,8-naphthalimide derivative is easy to prepare, and is an enhanced Cu2+ fluorescent probe, which can detect Cu2+ by two wavelengths and be applied to almost-all-water systems. According to atitration experiments and blank experiments at 392 nm and 754 nm, the detection limit of the 1,8-naphthalimide derivative of the present invention for Cu2+ is 2.6368×10−7 mol / L and 2.0156×10−7 mol / L, respectively, indicating that same can perform quantitative detection for Cu2+ with a high selectivity and a high sensitivity by using two wavelengths. In addition, a pH colorimetric switch based on 1,8-naphthalimide can rapidly and reversibly respond to a pH by means of three ways: a maximum absorption wavelength, absorbance and color change. Same has a narrow switching pH range, a good selectivity and a high sensitivity, can be used in almost-all-water systems.

The invention pertains to a method for preparing derivatives of the pyrazolinylnaphthalic acid having the general formula where Ar1 and Ar2 are unsubstituted or substituted phenyl radicals bearing in the para position an alkylated or acylated oxy- or amino group, or a polynuclear aryl radical, and Ar3 is a substituted N-naphthalimid or 1,8-naphthylene-1',2'-benzimidazole. Compounds ofthe above general formula are high-efficient red organic luminophors and are used widely as luminescent components of dyes for plastics and liquid scintillators, in hydrogeology to study water streams, to label the chemical industry wastewaters, as laser dyes, etc.