- First total synthesis of mariamide A
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Mariamide A, a lignanamide isolated from the seeds of Silybum marianum, has demonstrated potential utility as an antioxidant and antidiabetic agent and possesses an 8-O-4′ neolignan skeleton. Herein, a first total synthesis of mariamide A is presented that proceeds in nine steps using vanillin as the starting material. The key steps for the preparation of mariamide A involve an I2-catalyzed bromomethoxylation of an alkene group, a nucleophilic substitution followed by a sequential elimination and a monoacylation reaction.
- Xia, Yamu,Chen, Chenglong,Li, Mengying,Zhou, Weizeng,Sun, Shuyu,Chu, Shanpeng,Wang, Hui
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Read Online
- Carbosilane Glycodendrimers for Anticancer Drug Delivery: Synthetic Route, Characterization, and Biological Effect of Glycodendrimer-Doxorubicin Complexes
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The complexity of drug delivery mechanisms calls for the development of new transport system designs. Here, we report a robust synthetic procedure toward stable glycodendrimer (glyco-DDM) series bearing glucose, galactose, and oligo(ethylene glycol)-modified galactose peripheral units. In vitro cytotoxicity assays showed exceptional biocompatibility of the glyco-DDMs. To demonstrate applicability in drug delivery, the anticancer agent doxorubicin (DOX) was encapsulated in the glyco-DDM structure. The anticancer activity of the resulting glyco-DDM/DOX complexes was evaluated on the noncancerous (BJ) and cancerous (MCF-7 and A2780) cell lines, revealing their promising generation- and concentration-dependent effect. The glyco-DDM/DOX complexes show gradual and pH-dependent DOX release profiles. Fluorescence spectra elucidated the encapsulation process. Confocal fluorescence microscopy demonstrated preferential cancer cell internalization of the glyco-DDM/DOX complexes. The conclusions were supported by computer modeling. Overall, our results are consistent with the assumption that novel glyco-DDMs and their drug complexes are very promising in drug delivery and related applications.
- Müllerová, Monika,Maciel, Dina,Nunes, Nádia,Wrobel, Dominika,Stofik, Marcel,?ervenková ?tastná, Lucie,Krupková, Alena,Cu?ínová, Petra,Nováková, Kate?ina,Bo?ík, Matěj,Maly, Marek,Maly, Jan,Rodrigues, Jo?o,Stra?ák, Tomá?
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p. 276 - 290
(2022/01/04)
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- Discovery of deoxyceramide analogs as highly selective ACER3 inhibitors in live cells
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Acid (AC), neutral (NC) and alkaline ceramidase 3 (ACER3) are the most ubiquitous ceramidases and their therapeutic interest as targets in cancer diseases has been well sustained. This supports the importance of discovering potent and specific inhibitors
- Bielsa, Núria,Casasampere, Mireia,Aseeri, Mazen,Casas, Josefina,Delgado, Antonio,Abad, José Luis,Fabriàs, Gemma
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- S1P1 AGONIST AND APPLICATION THEREOF
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The present invention relates to a class of tricyclic compounds and an application thereof as a sphingosine 1-phosphate type 1 (S1P1) receptor agonist. The invention specifically relates to a compound represented by formula (II), and a tautomer and pharmaceutically acceptable salt of same.
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Paragraph 0345; 0349-0351
(2021/10/02)
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- COMPOSITIONS AND METHODS OF MODULATING SHORT-CHAIN DEHYDROGENASE ACTIVITY
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Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors described herein.
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- Synthesis of (3-(2-aminopyrimidin-4-yl)-4-hydroxyphenyl)phenyl methanone analogues as inhibitors of vascular endothelial growth factor receptor-2 kinase
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Angiogenesis is critical for tumor growth and mediated mainly by vascular endothelial growth factor (VEGF) signaling. Inhibition of the VEGF signaling pathway has emerged as one of the promising approaches for cancer therapy. VEGF receptor 2 (VEGFR-2) is
- More, Kunal N.,Lee, Jinho
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- First total synthesis of quiquesetinerviusin A
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The first total synthesis of the dihydrobenzofuran neolignan quiquesetinerviusin A and its related structure have been described. Phenolic coupling is the key step to constructing the dihydrobenzofuran skeleton with vanillin as the raw material. The hydroxyl group was protected with dihydropyran (DHP) and the ester group was reduced with diisobutylaluminium hydride (DIBAL-H) in order to obtain the crucial intermediate diol, which was then condensed with an acid ligand to give the desired compounds following removal of the protecting groups.
- Xia, Yamu,Mo, Zhen,Sun, Lin,Zou, Lijia,Zhang, Wen,Zhang, Jiahong,Wang, Lihong
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p. 296 - 300
(2017/06/19)
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- Rhodium-Catalyzed Decarbonylative Borylation of Aromatic Thioesters for Facile Diversification of Aromatic Carboxylic Acids
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Transformation of aromatic thioesters into arylboronic esters was achieved efficiently using a rhodium catalyst. The broad functional-group tolerance and mild conditions of the method have allowed for the two-step decarboxylative borylation of a wide range of aromatic carboxylic acids, including commercially available drugs.
- Ochiai, Hidenori,Uetake, Yuta,Niwa, Takashi,Hosoya, Takamitsu
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supporting information
p. 2482 - 2486
(2017/02/23)
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- Compound has the negative light dispersion, negative dispersion of this compound-containing composition and containing the composition for preparing anisotropic optical (by machine translation)
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The invention relates to a kind of reverse wdxrf compound, containing the compound reverse of wavelength dispersion composition and containing the optical anisotropic body. According to the present invention the reverse of wavelength dispersion composition is capable of providing a stronger and more stable reverse wdxrf nature, and can offer excellent optical performance of the optical anisotropic body. (by machine translation)
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Paragraph 0352; 0353
(2016/10/09)
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- COMPOUNDS HAVING NEGATIVE OPTICAL DISPERSION, NEGATIVE OPTICAL DISPERSION COMPOSITION COMPRISING THE COMPOUNDS, AND OPTICALLY ANISOTROPIC BODY COMPRISING THE COMPOSITION (As Amended)
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The present invention relates to a reverse wavelength dispersion compound, a reverse wavelength dispersion composition including the same, and an optically anisotropic body including the same. The reverse wavelength dispersion composition according to the present invention can provide a stronger and more stable reverse wavelength dispersion property, and makes it possible to provide an optically anisotropic body having excellent optical properties.
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Paragraph 0232
(2016/08/17)
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- COMPOSITION FOR MANUFACTURING OPTICAL ELEMENTS WITH NEGATIVE OPTICAL DISPERSION AND OPTICALLY ANISOTROPIC BODY MANUFACTURED THEREFROM
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The present invention relates to a composition for manufacturing optical elements with negative optical dispersion, and an optically anisotropic body prepared therefrom. According to the present invention, the optically anisotropic body showing stable reverse wavelength dispersion can be prepared more simply by using the composition for optical elements, and it is possible to apply the same to liquid crystal display devices as an optical film such as a thin-layer broadband λ/4 plate.
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Paragraph 0237
(2017/04/26)
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- IMPROVED PROCESS FOR MAKING DUOCARMYCIN PRODRUGS
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The present invention relates to a process comprising converting a compound of formula (I) into a compound of formula (II) by reaction with an organolithium reagent, which compound can be further converted into duocarmycin analogues consisting of a DNA- alkylating and a DNA-binding part, and still further into corresponding antibody-drug conjugates.
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- Synthetic method of kaempferol-3,7-β-D-bisglucoside and use thereof
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The purpose of the present invention is to provide a method for chemically synthesizing Kaempferol-3,7-β-D-bisglucoside which has effects of antioxidant, anticancer, etc to be industrially utilized. The present invention relates to a method for chemically synthesizing Kaempferol-3,7-β-D-bisglucoside in quantity, and uses thereof.
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Paragraph 0054; 0057; 0058
(2020/03/31)
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- Polymerizable liquid crystal compound, and optical antisotropic compsn.
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The present description relates to a polymerizable liquid crystal compound, a polymerizable liquid crystal composition including the same, and an optically anisotropic body. The polymerizable liquid crystal compound includes a radical derived from the first liquid crystal molecule including a mesogen group having a non-aromatic ring; a radical derived from the second liquid crystal molecule including a mesogen group that has a structure different from said mesogen group having a non-aromatic ring and includes a ring containing a double bond; and a linker that has a specific structure and links the sp3-hybridized carbon in the non-aromatic ring of the radical derived from the first liquid crystal molecule and the sp2-hybridized carbon in the mesogen group of the radical derived from the second liquid crystal molecule, wherein at least one of the radicals derived from the first and the second liquid crystal molecules may include one or more polymerizable groups which are connected to the mesogen group directly or via spacer groups. Such polymerizable liquid crystal compound makes it possible to exhibit stable reverse wavelength dispersion solely or by being mixed with other liquid crystal materials.
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Paragraph 0070
(2016/10/10)
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- JAK INHIBITOR
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A JAK inhibitor comprising, as an active ingredient, a nitrogen-containing heterocyclic compound represented by formula (I) {wherein W represents a nitrogen atom or -CH-; X represents -C (=O) - or -CHR4- (wherein R4 represents a hydrogen atom, or the like); R1 represents the formula described below [wherein Q1 represents-CR8-(wherein R8 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like); Q2 represents -NR15- (wherein R15 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like); and R5 and R6 may be the same or different and each represents a hydrogen atom, halogen, carboxy, substituted or unsubstituted lower alkyl, or the like], or the like; and R2 and R3 may be the same or different and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like} or a pharmaceutically acceptable salt thereof.
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Page/Page column 122
(2009/10/21)
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- NOVEL 3-(2-AMINO-4-PYRIMIDINYL)-4-HYDROXYPHENYL KETONE DERIVATIVES
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The present invention relates to novel compounds having 3-(2-amino-4-pyrimidinyl)-4-hydroxyphenyl ketone structure, as being illustrated in Formula 1, for inhibition of angiogenesis receptor tyrosine kinases, in particular, VEGF receptor 2 kinase ("KDR")
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- ARYL SULFAMATE DERIVATIVES
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The present invention provides an aryl sulfamate derivative represented by Formula (I) (wherein Rr and Rs, which may be the same or different, each represent a hydrogen atom or lower alkyl, R1, R2, R3
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- Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits
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A series of analogues of the protein kinase C (PKC) inhibitory natural product balanol which bear modified benzophenone subunits are described. The analogues were designed with the goal of uncovering structure -activity features that could be used in the development of PKC inhibitors with a reduced polar character compared to balanol itself. The results of these studies suggest that most of the benzophenone features found in the natural product are important for obtaining potent PKC inhibitory compounds. However, several modifications were found to lead to selective inhibitors of the related enzyme protein kinase A (PKA), and several specific modifications to the polar structural elements of the benzophenone were found to provide potent PKC inhibitors. In particular, it was found that replacement of the benzophenone carboxylate with bioisosteric equivalents could lead to potent analogues. Further, a tolerance for lipophilic substituents on the terminal benzophenone ring was uncovered. These results are discussed in light of recently available structural information for PKA.
- Lampe, John W.,Jagdmann Jr., G. Erik,Johnson, Mary George,Lai, Yen-Shi,Lowden, Christopher T.,Lynch, Michael P.,Mendoza, José S.,Murphy, Marcia M.,Wilson, Joseph W.,Ballas, Lawrence M.,Carter, Kiyomi,Biggers, Christopher K.,Darges, James W.,Davis, Jefferson E.,Hubbard, Frederick R.,Stamper, Mark L.,Defauw, Jean M.,Foglesong, Robert J.,Hall, Steven E.,Heerding, Julia M.,Hollinshead, Sean P.,Hu, Hong,Hughes, Philip F.
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p. 2624 - 2643
(2007/10/03)
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- Glucopyranoside recognition by polypyridine-macrocyclic receptors possessing a wide cavity with a flexible linkage
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New polypyridine-macrocyclic receptors for glucopyranosides were designed and synthesized. The artificial receptors possess a terpyridine skeleton as a hydrogen-bonding site and a flexible polyoxyethylene chain as a bridge for the macrocyclic structure, in which the cavity of the receptors is large enough to incorporate pyranosides. The receptors showed high affinities for n-octyl ?2-(D)-glucopyranoside, and selective binding of the receptors was observed between epimeric pyranosides. The results obtained in this paper demonstrated versatility of the terpyridine skeleton as a hydrogenbonding site for saccharides.
- Inouye, Masahiko,Chiba, Junya,Nakazumi, Hiroyuki
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p. 8170 - 8176
(2007/10/03)
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- Prediction of the Absolute Configuration of Optically Active Pheromones Using Liquid Crystals
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Prediction of the absolute configuration of optically active methyl branched pheromones is possible by combining them with mesogens to give them liquid crystalline properties and measuring the helical senses of the chiral nematic phases.
- Ikemoto, Tetsuya,Mitsuhashi, Kazuhiro,Mori, Kenji
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p. 687 - 694
(2007/10/02)
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