- Novel compound and application thereof in preparation of medicine for treating cancer
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The invention provides a novel compound and application thereof in preparation of a medicament for treating cancer. The compound has the activity of promoting PSGR expression in the prostate cancer cells, can activate PSGR signals, has the effect of inhibiting the proliferation of prostate cancer cells, is expected to be applied to treating prostatic cancer in the future and is a potential medicine for treating prostatic cancer. In addition, the inventors have unexpectedly found that compounds satisfying the above conditions have been expected to have activity to inhibit proliferation of breast cancer cells and ovarian cancer cells in addition to the activity of inhibiting proliferation of prostate cancer cells, and are expected to be potential drugs for treating breast cancer and ovarian cancer. A wide clinical application prospect is shown.
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Paragraph 0114-0116
(2021/10/11)
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- Preparation method of anti-aging agent AW
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The invention belongs to the technical field of fine chemical engineering and relates to an anti-aging agent AW and a preparation method thereof. An anti-aging agent AW crude product is prepared under the action of a catalyst by taking p-aminobenzene ethyl ether and acetone as raw materials. AW G of the crude product was taken up, and the reaction was performed. When the oxidizing agent is an acidic substance, the liquid base is added and neutralized, the pH is adjusted pH to 10 - 12, the liquid is separated, the oil phase is washed, and the low-amine AW finished product is obtained by rectification. The content of the product AW prepared by the method can reach 99.5-99 .9%, the primary amine content is reduced to within 40 ppm, and the safety of the product is greatly improved. Compared with the prior art, the process operation is simple, the cost is increased, and the product quality is excellent.
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Paragraph 0027-0031
(2021/08/25)
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- A surface-active ionic liquid catalyst used for the synthesis of ethoxy quinoline (by machine translation)
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The invention relates to a with the surface activity of the ionic liquid catalyst used for the synthesis of ethoxy quinoline, which belongs to the field of chemical synthesis. The activity of the catalyst is the surface of the ionic liquid, the catalyst the catalytic activity is high, good stability, catalytic reaction time is short, the one-way high conversion rate, the catalyst is easy to recovery can be recycled; and the catalyst is also used as a solvent, without additional adding the reaction solvent. The method improves production efficiency, reduces the energy consumption of the production. (by machine translation)
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Paragraph 0019-0026
(2019/10/23)
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- METHOD FOR SYNTHESIZING HIGH PURITY ETHOXYQUIN, HIGH PURITY ETHOXYQUIN SYNTHESIZED BY THE SAME AND ANTIOXIDANT FOR FEED SUPPLEMENT INCLUDING THE SAME
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The present invention relates to a synthesis method of high-purity ethoxyquin, high-purity ethoxyquin synthesized thereby, and an antioxidant agent for use in a feed additive comprising the same. The synthesis method of high-purity ethoxyquin according to the present invention comprises: (S100) weighing of a first raw material and introduction of the same into a reactor step for weighing a first raw material and introducing the first raw material into a reactor; (S200) a heating step for heating the reactor in which the first raw material and a catalyst have been introduced; (S300) a second raw material introduction and reaction step for introducing a second raw material into the heated reactor to conduct a reaction of the first raw material and the second raw material; (S400) a cooling, neutralization and separation step for cooling and neutralizing a product produced from progression of the reaction inside the reactor and separating the product; and (S500) a distillation step for distilling the separated product to produce an ethoxyquin monomer. Through the above configuration, the antioxidant agent for use in a feed additive comprising high-purity ethoxyquin according to the present invention can prevent nutrients from being destroyed due to fatty acid oxidation; prevents degradation of nutrients due to storage of raw materials, and distribution and storage of a feed to prevent degradation in quality of the feed; and maintain the quality and freshness of the feed uniformly for a long time.(S100) Weighing of a first raw material and introduction of the same into a reactor step(S200) Heating step(S300) Second raw material introduction and reaction step(S400) Cooling, neutralization and separation step(S500) Distillation stepCOPYRIGHT KIPO 2018
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Paragraph 0092-0096
(2018/05/15)
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- New fluorescence-based high-throughput screening assay for small molecule inhibitors of tyrosyl-DNA phosphodiesterase 2 (TDP2)
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Tyrosyl-DNA phosphodiesterase 2 (TDP2) repairs topoisomerase II (TOP2) mediated DNA damages and causes resistance to TOP2-targeted cancer therapy. Inhibiting TDP2 could sensitize cancer cells toward TOP2 inhibitors. However, potent TDP2 inhibitors with favorable physicochemical properties are not yet reported. Therefore, there is a need to search for novel molecular scaffolds capable of inhibiting TDP2. We report herein a new simple, robust, homogenous mix-and-read fluorescence biochemical assay based using humanized zebrafish TDP2 (14M_zTDP2), which provides biochemical and molecular structure basis for TDP2 inhibitor discovery. The assay was validated by screening a preselected library of 1600 compounds (Z′ ≥ 0.72) in a 384-well format, and by running in parallel gel-based assays with fluorescent DNA substrates. This library was curated via virtual high throughput screening (vHTS) of 460,000 compounds from Chembridge Library, using the crystal structure of the novel surrogate protein 14M_zTDP2. From this primary screening, we selected the best 32 compounds (2% of the library) to further assess their TDP2 inhibition potential, leading to the IC50 determination of 10 compounds. Based on the dose-response curve profile, pan-assay interference compounds (PAINS) structure identification, physicochemical properties and efficiency parameters, two hit compounds, 11a and 19a, were tested using a novel secondary fluorescence gel-based assay. Preliminary structure-activity relationship (SAR) studies identified guanidine derivative 12a as an improved hit with a 6.4-fold increase in potency over the original HTS hit 11a. This study highlights the importance of the development of combination approaches (biochemistry, crystallography and high throughput screening) for the discovery of TDP2 inhibitors.
- Ribeiro, Carlos J.A.,Kankanala, Jayakanth,Shi, Ke,Kurahashi, Kayo,Kiselev, Evgeny,Ravji, Azhar,Pommier, Yves,Aihara, Hideki,Wang, Zhengqiang
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- Preparation method of ethoxyquin
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The invention discloses a preparation method of ethoxyquin. The method comprises the following concrete steps: 1, enabling 4-ethoxy-N-(propane-2-alkenyl)aniline, which is taken as a raw material, to react with ((2-methyl-1,3-dioxolane-2-yl)methyl)magnesium chloride to obtain an intermediate product; 2, hydrolyzing the obtained intermediate product for deprotection; 3, enabling the hydrolyzed product to make a cyclization reaction under an acidic condition to prepare the ethoxyquin. The ethoxyquin is prepared by a one-step method, the intermediate produced in the preparation process does not need to be separated, and a great deal of acetone and methylbenzene are not needed by the reaction, so that the conversion rate of the raw material is better improved, a reaction solvent is saved, and the pressure of environmental protection is reduced; the preparation method has the advantages of mild reaction conditions, simple technology, convenient operation and environment friendliness; furthermore, the obtained product is also higher in purity and can meet the demands of feed markets at all levels, thus having better industrial prospect.
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Paragraph 0012; 0013; 0014; 0015; 0016; 0017; 0018-0026
(2017/08/29)
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- A method of synthesizing ethoxy quinoline
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The invention relates to a method for synthesizing ethoxyquinoline, belonging to the fields of feed and food. The method comprises the following steps: 1) synthesis; 2) filtration; 3) washing; and 4) distillation. The acetic anhydride used as the solvent can enhance the reaction conversion rate; and the acetic anhydride can also be used as a water-carrying agent. The synthesis reaction is reversible reaction. The acetic anhydride used as the water-carrying agent can carry water generated by reaction away along with the volatilization of the acetic anhydride in the heating reaction process, thereby enhancing the reaction conversion rate. Cuprous chloride used as a catalyst exists in the reaction process in the form of solid, and can be separated and recycled without extraction after the reaction finishes. Under the interactions of the acetic anhydride solvent and cuprous chloride catalyst, the synthesis reaction method has the advantages of high reaction rate, higher conversion rate, low consumption of the solvent and catalyst, low raw material cost and no pollution, and the synthesized ethoxyquinoline can satisfy the feed-grade requirements.
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Paragraph 0023; 0044-0053
(2017/02/23)
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- 2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway
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Synthesis and SAR investigation of 2-guanidinoquinazolines, initially identified in a high content screen for selective STAT3 pathway inhibitors, led to a more potent analog (11c) that demonstrated improved anti-proliferative activity against a panel of HNSCC cell lines.
- Laporte, Matthew G.,Da Paz Lima, Dimas Jos,Zhang, Feng,Sen, Malabika,Grandis, Jennifer R.,Camarco, Daniel,Hua, Yun,Johnston, Paul A.,Lazo, John S.,Resnick, Lynn O.,Wipf, Peter,Huryn, Donna M.
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supporting information
p. 5081 - 5085
(2014/12/11)
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- C-N coupling of 1,2-dihydro-2,2,4-trimethylquinoline derivatives via a silver(I)-catalyzed direct functionalization of a C-H bond
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Two C,N-linked dimeric 1,2-dihydro-2,2,4-trimethylquinolines, namely 6-chloro-1-(6-chloro-1,2-dihydro-2,2,4-trimethylquinolin-8-yl)-1,2-dihydro-2,2, 4-trimethylquinoline (3a) and 6-ethoxy-1-(6-ethoxy-1,2-dihydro-2,2,4- trimethylquinolin-8-yl)-1,2-dihydro-2,2,4-trimethylquinoline (3b), have been prepared through a silver-catalyzed dimerization of their corresponding monomers. The effect of different silver salts on the reaction was also investigated, and the obtained results suggest that silver ions effectively catalyzed the formation of a C-N bond under these mild conditions. This represents one of the rare reports on the silver-catalyzed C-N bond formation through a coupling of a secondary amine and an activated aromatic system, via a direct C-H functionalization. Theoretical studies showed that these dimeric structures favor a conformation in which their monomer units are oriented approximately perpendicular to each other, with an intramolecular hydrogen bond (N-H distance of 2.33 A) forming between the hydrogen atom of the amine in one of the monomeric units and the tertiary nitrogen atom of the other one.
- Fotie, Jean,Rhodus, Jessica L.,Taha, Hashem A.,Reid, Carolyn S.
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p. 598 - 604
(2013/01/15)
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- Induction of chromosome aberrations in cultured human lymphocytes treated with ethoxyquin
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The chromosomal aberration test was employed to investigate the effect in vitro of a known antioxidant and food preservative, ethoxyquin (EQ, 1,2-dihydro-6-ethoxy-2,2,4-trimethylquinoline) on human chromosomes. The studies were undertaken because there are no published in vitro data on genotoxicity of EQ in mammalian cells and there are many reports pointing out that it may be harmful to animals and human beings. Lymphocytes obtained from three healthy donors were incubated with EQ (0.01-0.5mM) both with and without metabolic activation. Stability studies performed by HPLC analysis showed that EQ was stable under the conditions of the lymphocyte cultures. The results of the chromosome aberration assay showed that EQ induces chromosome aberrations: gaps and breaks as well as dicentrics and atypical translocation chromosomes.
- Blaszczyk,Osiecka,Skolimowski
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p. 117 - 128
(2007/10/03)
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- Palatable solid pesticidal compositions of ethylene and vinyl acetate copolymer
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The invention comprises compositions in solid form of ethylene/vinyl acetate copolymer with an effective amount of bioactive agent, a protein/carbohydrate-lipid source, 0 to 20% of an edible oil and optionally an attractant, dye, preservative, adversive agent and biomarker and the use, thereof, to control pests.
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- Long-acting pyrethrum/pyrethroid based pesticides with silicone stabilizers
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Pesticidal compositions based on nontoxic, naturally unstable insecticides (pyrethrum, synthetic pyrethroids and mixtures thereof) include a liquid alkyl aryl silicone polymer which stabilizes the insecticide to provide an extended effective killing life. The compositions additionally include a synergist to provide an immediate killing action and an antioxidant to protect the insecticide against destruction by oxygen. Ultraviolet protectants and insect repellents may also be included. Applications include control of insect pests to animals and plants and general purpose insect control. Exemplary formulations are given for compositions to be applied as sprays, dips, powdered or dusts, foggers and shampoos.
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- Nickel stabilizers for synthetic polymers
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New complexes of nickel salts of hydroxybenzoic acids are stabilizers for polymers. The complexes are prepared by reacting a nickel benzoate with a corresponding alcohol.
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- Piperidine derivatives
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A composition comprising an organic material and, as stabiliser, a compound having the formula SPC1 And salts thereof, wherein R1 and R2 are the same or different and each is an alkyl residue having from 1 to 12 carbon atoms or R1 and R2, together with the carbon atom to which they are bound, form a cycloalkyl residue having from 5 to 12 carbon atoms in the ring, Y is O, hydrogen, a straight or branched alkyl residue having from 1 to 20 carbon atoms, an alkenyl or alkynyl residue having from 3 to 12 carbon atoms, an aralkyl residue having from 7 to 12 carbon atoms or a group having the formula EQU1 wherein R is hydrogen, or a methyl or phenyl residue and R3 is hydrogen or a straight- or branched chain alkyl residue having from 1 to 12 carbon atoms.
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