- Phosphine-catalyzed sequential (2+3)/(2+4) annulation of γ-vinyl allenoates: Access to the synthesis of chromeno[4,3-: B] pyrroles
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A phosphine-catalyzed cascade (2+3)/(2+4) cyclization reaction of γ-vinyl allenoates with aldimine esters has been developed to provide a series of chromeno[4,3-b]pyrrole derivatives that contain three contiguous stereogenic centers. The method gives a good yield, excellent chemoselectivity and diastereoselectivity under mild conditions.
- Huang, You,Li, Xiaohu
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supporting information
p. 9934 - 9937
(2021/10/12)
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- Cytotoxicity of new pyridazin-3(2H)-one derivatives orchestrating oxidative stress in human triple-negative breast cancer (MDA-MB-468)
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Triple-negative breast cancer (TNBC) is a complex and aggressive subtype of breast cancer characterized by high morbidity and mortality. In the absence of targeted therapy, only chemotherapy is available in this case of cancer. The current study investigated the antitumor effect of new pyridazin-3(2H)-one derivatives on the human TNBC cell line, MD-MB-468. The in vitro cytotoxic activities were investigated using the tetrazolium-based MTT assay. Lipid peroxidation, H2O2 content, and the specific activities of antioxidant enzymes were also determined. Two molecules, 6f and 7h, were found to be selectively highly active against tumor cells with IC50 values of 3.12 and 4.9 μM, respectively. Furthermore, cells exposed to 6f showed a significant increase in H2O2 and lipid peroxidation levels, accompanied by a decrease in the enzyme activities of glutathione reductase (GR) and thioredoxin reductase (TrxR). The cytotoxicity of the compound 6f may improve the therapeutic efficacy of the current treatment for TNBC via the inhibition of GR and TrxR activities.
- Bouchmaa, Najat,Ben Mrid, Reda,Boukharsa, Youness,Nhiri, Mohamed,Ait Mouse, Hassan,Taoufik, Jamal,Ansar, M'hammed,Zyad, Abdelmajid
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- Design and synthesis of novel Vitamin D-coumarin hybrids using microwave irradiation
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A series of novel vitamin D-coumarin hybrids were synthesised by esterification of the corresponding coumarin-3-carboxylic acids and vitamin D or vitamin D CD-ring alcohol in CH2Cl2 under microwave irradiation. They were obtained in higher yields (from 64-81% up to 79-87%) and shorter reaction time (from 3 h down to 15 min), compared with earlier conventional methodologies. The structures of all the target compounds were confirmed by 1H NMR, 13C NMR and HRMS. This provides an attractive and alternative method for the preparation of high-value vitamin D-coumarin hybrids.
- Zhang, Hengrui,Fang, Zhijie
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p. 684 - 687
(2018/01/08)
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- Synthesis characterization and cytotoxicity studies of platinum(II) complexes with reduced amino pyridine schiff base and its derivatives as ligands
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A series of reduced amino pyridine Schiff base platinum(II) complexes were prepared as potential anticancer drugs, and characterized by NMR, IR spectroscopy, elemental analysis, and molar conductivity. UV and CD results showed the binding mode between these compounds and salmon sperm DNA may be intercalation. The cytotoxicity of these complexes was validated against A549, Hela, and MCF-7 cell lines by MTT assay. Some complexes exhibited better cytotoxic activity than cisplatin against Hela and MCF-7 cell lines.
- Li, Li-Jun,Yan, Qin-Qin,Liu, Guo-Jun,Yuan, Zhen,Lv, Zhen-Hua,Fu, Bin,Han, Yan-Jun,Du, Jian-Long
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p. 1081 - 1089
(2017/05/29)
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- NO-RELEASING NITROOXY-CHROMENE CONJUGATES
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The present invention provides NO-releasing nitrooxy-alkylenyl-linked-chromene conjugates, having the structure of Formula (1) wherein R1, R2, R3, R4, X, and L are as defined in the detailed description; pharmaceutical compositions comprising at least one compound o Formula (I); and methods useful for healing wounds, preventing and treating cancer and treating actinic keratosis, cystic fibrosis, and acne, using a compound of Formula (1).
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Paragraph 0295; 0296
(2016/12/16)
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- NO-RELEASING NITROOXY-CHROMENE CONJUGATES
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The present invention provides NO-releasing nitrooxy-alkylenyl-linked-chromene conjugates, having the structure of Formula (1 ) wherein R1, R2, R3, R4, X, and L are as defined in the detailed description; pharmaceutical compositions comprising at least one compound o Formula (I); and methods useful for healing wounds, preventing and treating cancer and treating actinic keratosis, cystic fibrosis, and acne, using a compound of Formula (1).
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Paragraph 0205; 0206
(2015/08/03)
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- NO-RELEASING NONOATE(OXYGEN-BOUND)CHROMENE CONJUGATES
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The present invention provides NO-releasing NONOate(oxygen bound)chromene conjugates, having the structure of Formula (I): wherein Z, R1, R2, R3, R4, R5, R6, and R7 are as defined in the detailed description; pharmaceutical compositions comprising at least one compound of Formula (I); and methods useful for healing wounds, preventing and treating cancer, or treating actinic keratosis, cystic fibrosis, or acne, using a compound of Formula (I).
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Paragraph 0204; 0205
(2015/08/03)
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- NO-RELEASING GUANIDINE-CHROMENE CONJUGATES
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The present disclosure provides NO-releasing guanidine-chromene conjugates, having the structure of Formula (I): wherein R1, R2, R3, R4, R10, and L are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds of Formula (I); and methods useful for healing wounds, preventing and treating cancer, or treating actinic keratosis, cystic fibrosis, acne, or a disease mediated by arginine deficiency using a compound of Formula (I).
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Paragraph 0263; 0264
(2015/07/22)
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- Cu-Mn spinel oxide catalyzed regioselective halogenation of phenols and N-heteroarenes
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A novel simple, mild chemo- and regioselective method has been developed for the halogenation of phenols using Cu-Mn spinel oxide as a catalyst and N-halosuccinimide as halogenating agent. In the presence of Cu-Mn spinel oxide B, both electron-withdrawing and electron-donating groups bearing phenols gave monohalogenated products in good to excellent yields with highest para-selectivity. The para-substituted phenol gave monohalogenated product with good yield and ortho-selectivity. N-Heteroarenes such as indoles and imidazoles also gave monohalogenated products with high selectivity. Unlike the copper-catalyzed halogenation, the present method works well with electron-withdrawing group bearing phenols and gives comparatively better yields and selectivity. The Cu-Mn spinel catalyst is robust and reused three times under optimized conditions without any loss in catalytic activity. Nonphenolics did not undergo this transformation.
- Singh, Parvinder Pal,Thatikonda, Thanusha,Kumar, K. A. Aravinda,Sawant, Sanghapal D.,Singh, Baldev,Sharma, Amit Kumar,Sharma,Singh, Deepika,Vishwakarma, Ram A.
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scheme or table
p. 5823 - 5828
(2012/09/05)
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- Non-metallocene compounds, method for the production thereof and use of the same for the polymerisation of olefins
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The invention relates to a method for producing special transition metal compounds, to novel transition metal compounds and to the use of the same for the polymerisation of olefins.
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- Method for producing optically active salicylaldimine copper complex
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There is provided a method for producing an optically active salicylaldimine copper complex, which method is characterized in that an optically active amino alcohol compound represented by the following formula (1) is reacted with copper hydroxide (II) in an organic solvent. wherein R1 and R2 which are the same or different, each represent lower alkyl groups and the like which may be substituted, X1 and X2 which are the same or different, each represent a hydrogen atom, lower alkyl groups and the like, and the symbol * designates an asymmetric carbon atom.
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- A Simple Method for the Preparation of Dichlorocatechols.
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Dichlorocatechols (DCC) are common metabolites in the aerobic degradation of dichlorobenzenes. Their synthesis is therefore possible either enzymatically, or chemically by several two-step-synthesis starting from cycloalkanones or suitable dichlorophenols. A modified ultrasonic Reimer/Tiemann reaction and subsequent Dakin oxidation was used to prepare 3,5-DCC and 4,5-DCC. A new UV-photoradical single step synthesis of 3,4-dichlorocatechol as well as 3,6-dichlorocatechol is described in detail. Mass spectral and 13C-NMR spectral data of all four dichlorocatechol isomers are presented.
- Kirsch, Nils H.,Stan, H.-J.
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p. 131 - 138
(2007/10/03)
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- Photochromatic compound, a method for its preparation, and articles which contain it
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A photochromatic compound represented by the following general formula (I): STR1 where: R1 and R2 independently represent a linear, branched or cyclic C1-C10 alkyl radical, H, OH, F, Cl, Br, NH2, N(R4)2, COOH, OR4 or COOR4 where R4 is a C1-C10 linear, branched or cyclic alkyl radical, or an aryl radical; R3 is a variously substituted mono or polycondensed heterocyclic or aryl radical. A compound (I) demonstrates marked photochromatic characteristics both when in an organic solvent solution and when incorporated into polymer matrices.
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- Photochromatic compound, a method for its preparation, and articles which contain it
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A photochromatic compound represented by the following general formula (I): where:, R1 and R2 independently represent a linear, branched or cyclic C1-C10 alkyl radical, H, OH, F, Cl, Br, NH2, N(R4)2, COOH, OR4 or COOR4 where R4 is a C1-C10 linear, branched or cyclic alkyl radical, or an aryl radical;, R3 is a variously substituted mono or polycondensed heterocyclic or aryl radical. A compound (I) demonstrates marked photochromatic characteristics both when in an organic solvent solution and when incorporated into polymer matrices.
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- Formylation of Phenols with Electron-withdrawing Groups in Strong Acids. Synthesis of Substituted Salicylaldehydes
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Salicylaldehydes with electron-withdrawing groups, i.e., 2-hydroxy-5-nitrobenzaldehyde (2a), methyl 3-formyl-4-hydroxybenzoate (2b), methyl 5-chloro-3-formyl-2-hydroxybenzoate (2c), 3,5-dichloro-2-hydroxybenzaldehyde (2d), 5-cyano-2-hydroxybenzaldehyde (2e), and 5-fluoro-2-hydroxybenzaldehyde (2f), were synthesized by the formylation of the corresponding phenols (1a-f) with hexamethylenetetramine in 75percent polyphosphoric acid, methanesulfonic acid, or trifluoroacetic acid.The yields of these reactions were better than those of the Duff reaction.Keywords-Duff reaction; formylation; hexamethylenetetramine; methanesulfonic acid; phenol; polyphosphoric acid; salicylaldehyde; trifluoroacetic acid
- Suzuki, Yuji,Takahashi, Hiroshi
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p. 1751 - 1753
(2007/10/02)
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- Metal complexes of bis-hydrazones
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Bis-hydrazone metal complexes of the formula STR1 wherein A denotes an isocyclic or heterocyclic radical, R denotes a H atom, an alkyl group or an aryl radical, M denotes a divalent transition metal and zinc or cadmium, X1 and X2 independently of one another represent alkyl, cycloalkyl, aralkyl or aryl radicals, or conjointly form a fused carbocyclic or heterocyclic aromatic ring, L denotes a ligand having one or more coordinating N or S atoms, and n denotes the number 1 - 5, are useful for coloring plastic and lacquers in fast yellow to red shades.
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- Azomethine pigments
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Azomethine pigments of the formula SPC1 And metal complexes thereof, wherein A denotes an isocyclic or heterocyclic aromatic radical, R denotes a H atom, an alkyl group containing 1-6 C atoms, or an aryl radical, X2 and X4 denote H atoms or halogen atoms, X1 and X3 denote H atoms or halogen atoms, alkoxy or alkylmercapto groups containing 1-6 C atoms, cycloalkoxy groups containing 5-6 C atoms, or aralkoxy, aryloxy or arylmercapto groups, it being possible for one of the substituents X1 -X4 also to be a nitro group which are useful for pigmenting of high molecular material.
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