- Robust onionlike structures with magnetic and photodynamic properties formed by a fullerene C60-POM hybrid
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We report for the first time the synthesis of a covalently-linked fullerene C60-Dawson POM hybrid, which can form onionlike structures with rich magnetic, electrochemical and photodynamic properties.
- Zhou, Shengju,Feng, Yongqiang,Chen, Mengjun,Li, Qian,Liu, Baoyong,Cao, Jiamei,Sun, Xiaofeng,Li, Hongguang,Hao, Jingcheng
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Read Online
- Discovery of Novel Dual-Target Inhibitor of Bromodomain-Containing Protein 4/Casein Kinase 2 Inducing Apoptosis and Autophagy-Associated Cell Death for Triple-Negative Breast Cancer Therapy
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Bromodomain-containing protein 4 (BRD4) is an attractive epigenetic target in human cancers. Inhibiting the phosphorylation of BRD4 by casein kinase 2 (CK2) is a potential strategy to overcome drug resistance in cancer therapy. The present study describes the synthesis of multiple BRD4–CK2 dual inhibitors based on rational drug design, structure–activity relationship, and in vitro and in vivo evaluations, and 44e was identified to possess potent and balanced activities against BRD4 (IC50 = 180 nM) and CK2 (IC50 = 230 nM). In vitro experiments show that 44e could inhibit the proliferation and induce apoptosis and autophagy-associated cell death of MDA-MB-231 and MDA-MB-468 cells. In two in vivo xenograft mouse models, 44e displays potent anticancer activity without obvious toxicities. Taken together, we successfully synthesized the first highly effective BRD4–CK2 dual inhibitor, which is expected to be an attractive therapeutic strategy for triple-negative breast cancer (TNBC).
- Chen, Juncheng,Chiang, Cheng-Ming,He, Gu,Liu, Bo,Liu, Jie,Ouyang, Liang,Tang, Pan,Wang, Guan,Yang, Chengcan,Ye, Tinghong,Zhang, Jifa,Zhang, Jin,Zou, Ling
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p. 18025 - 18053
(2022/01/03)
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- Supramolecular Assemblies for Transporting Proteins Across an Immiscible Solvent Interface
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Polymeric supramolecular assemblies that can effectively transport proteins across an incompatible solvent interface are described. We show that electrostatics and ligand-protein interactions can be used to selectively transport proteins from an aqueous phase to organic phase. These transported proteins have been shown to maintain their tertiary structure and function. This approach opens up new possibilities for application of supramolecular assemblies in sensing, diagnostics and catalysis.
- Gao, Jingjing,Zhao, Bo,Wang, Meizhe,Serrano, Mahalia A. C.,Zhuang, Jiaming,Ray, Moumita,Rotello, Vincent M.,Vachet, Richard W.,Thayumanavan
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supporting information
p. 2421 - 2425
(2018/02/28)
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- BENZO- OR PYRIDO-IMIDAZOLE DERIVATIVE
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The present invention addresses the problem of finding a compound having both PPAR activation activity and angiotensin receptor antagonistic activity. The present invention is a benzo- or pyrido-imidazole derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, or a ester or amide thereof (where A is biphenyl methyl-imidazolyl, biphenyl methyl-benzimidazolyl, or the like, B is divalent benzimidazolyl or the like, C is carboxyl or the like, E is divalent phenyl, naphthyl, or the like, G is a dangling bond, oxygen, or the like, Q is oxygen or sulfur, n is an integer from 1 to 6, p is an integer from 1 to 6, V is a dangling bond, oxygen, or the like, and R is hydrogen, alkyl, or the like).
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Paragraph 0665; 0666
(2013/04/25)
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- Adenosine A2A receptor-antagonist/dopamine D2 receptor-agonist bivalent ligands as pharmacological tools to detect A 2A-D2 receptor heteromers
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Adenosine A2A (A2AR) and dopamine D2 (D2R) receptors mediate the antagonism between adenosinergic and dopaminergic transmission in striatopallidal GABAergic neurons and are pharmacological targets for the treatment of Parkinson's disease.Here, a family of heterobivalent ligands containing a D2R agonist and an A 2AR antagonist linked through a spacer of variable size was designed and synthesized to study A2AR-D2R heteromers. Bivalent ligands with shorter linkers bound to D2R or A2AR with higher affinity than the corresponding monovalent controls in membranes from brain striatum and from cells coexpressing both receptors. In contrast, no differences in affinity of bivalent versus monovalent ligands were detected in experiments using membranes from cells expressing only one receptor. These findings indicate the existence of A2AR-D2R heteromers and of a simultaneous interaction of heterobivalent ligands with both receptors. The cooperative effect derived from the simultaneous interaction suggests the occurrence of A2AR-D2R heteromers in cotransfected cells and in brain striatum. The dopamine/adenosine bivalent action could constitute a novel concept in Parkinson's disease pharmacotherapy.
- Soriano, Aroa,Ventura, Ruben,Molero, Anabel,Hoen, Rob,Casado, Vicent,Corte, Antoni,Fanelli, Francesca,Albericio, Fernando,Lluís, Carmen,Franco, Rafael,Royo, Miriam
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supporting information; experimental part
p. 5590 - 5602
(2010/03/24)
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- RADIATION-SENSITIVE COMPOSITION
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A radiation-sensitive composition containing a resist compound having a high sensitivity, a high resolution, a high etching resistance, and a low outgas which forms a resist pattern with a good shape is described. Further described is a method of forming a resist pattern using the radiation-sensitive composition. Still further described are a novel composition for forming a photoresist under coat film which is excellent in optical properties and etching resistance and contains substantially no sublimable substance and an under coat film formed by the composition. Still further described are a radiation-sensitive composition containing a solvent and a cyclic compound having a specific structure, for example, a cyclic compound (A) having a molecular weight of 700 to 5000 which is synthesized by the condensation reaction of a compound having 2 to 59 carbon atoms and 1 to 4 formyl groups (aldehyde compound (A1)) with a compound having 6 to 15 carbon atoms and 1 to 3 phenolic hydroxyl groups (phenol compound (A2)), and a cyclic compound for use in the radiation-sensitive composition.
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Page/Page column 111-112
(2009/08/14)
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- SWALLOWTAIL MOTIFS FOR IMPARTING WATER SOLUBILITY TO PORPHYRINIC COMPOUNDS
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Porphyrinic compounds that contain solubilizing groups are described, along with methods of making and using the same and compositions comprising such compounds. Examples of such compounds include compounds compounds of Formula (I) wherein: Z is a porphyr
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Page/Page column 72-73; 87-88
(2008/06/13)
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- HYDRAZONE DERIVATIVE
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A compound represented by the following formula (I): wherein R1 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R2 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R3 represents hydrogen, etc.; Ar represents a divalent group derived from aromatic hydrocarbon, etc.; X represents a single bond, linear or branched alkylene having from 1 to 3 carbon atoms which may have a substituent, etc.; and G represents halogen, a saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc., a salt thereof or a solvate thereof; and an agent for inhibiting aggregation and/or deposition of an amyloid protein or an amyloid-like protein, which comprises the compound, a salt thereof or a solvate thereof
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Page/Page column 127
(2010/11/08)
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- Selective MMP-13 inhibitors
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The invention relates to a pyrimidine-4,6-dicarboxylic acid diamide compound, pharmaceutical preparation comprising it, process for preparing it and method for its pharmaceutical use. Particularly, the pyrimidine-4,6-dicarboxylic acid diamide compound is
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Page/Page column 8
(2010/02/10)
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- DIPHENYLAZETIDINONE DERIVATES POSSESSING CHOLESTEROL ABSORPTION INHIBITORY ACTIVITY
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Compounds of formula (I) (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described. Processes for their manufacture and pharmaceutical compositions containing them are also described.
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Page/Page column 149
(2010/02/12)
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- INDOLINONE DERIVATIVES AS RECEPTOR TYROSINE KINASE IHIBITORS
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Novel derivatives of compound (E)-1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-2H-indol-2-one and the use thereof for the preparation of medicaments for the treatment of tumors in which the tyrosine kinase activity proteins Met, PDGF-R, FGF-R1
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Page/Page column 32-33
(2008/06/13)
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- Indolinone derivatives
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Novel derivatives of compound (E)-1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-2H-indol-2-one and the use thereof for the preparation of medicaments for the treatment of tumors in which the tyrosine kinase activity proteins Met, PDGF-R, FGF-R1
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Page/Page column 15
(2008/06/13)
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- Partially protected novel trisphenols and process for production thereof
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The invention provides a partially protected trisphenol having the general formula (I) wherein R1is an alkyl group of 1-4 carbons or an alkoxyl group of 1-4 carbons, R2is an alkyl group of 1-6 carbons or a cycloalkyl group of 5 or 6 carbons, X1is a hydrogen atom, an alkoxycarbonylmethyl group wherein the alkyl group has 1-4 carbons, an alkoxycarbonyl group wherein the alkyl group has 1-4 carbons or a tetrahydropyranyl group, X2is a hydrogen atom, an alkoxycarbonylmethyl group wherein the alkyl group has 1-4 carbons, an alkoxycarbonyl group wherein the alkyl group has 1-4 carbons or a tetrahydropyranyl group, provided that when X1is a hydrogen atom, X2is not a hydrogen atom, and when X2is a hydrogen atom, X1is not a hydrogen atom; and m is an integer of 0, 1 or 2, and n is an integer of 0, 1, 2 or 3.
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- Propionic acid derivatives
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The present application relates to novel potent PPAR-alpha-activating compounds for treating, for example, coronary heart disease, and to their preparation.
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- 4- AND 5-ALKYNYLOXINDOLES AND 4- AND 5-ALKENYLOXINDOLES
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4- and 5-alkynyloxindoles as well as 4- and 5-alkenyloxindoles having formula (I) and (II), wherein R, R, R, R, R, X and z have the meaning indicated in the specification, inhibit or modulate protein kinases, in particular JNK protein kinases and are useful as anti-inflammatory agents, particularly in the treatment of rheumatoid arthritis.
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Page/Page column 37; 38
(2010/02/04)
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- 4-and 5-alkynyloxindoles and 4-and 5-alkenyloxindoles
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Disclosed are 4- and 5-alkynyloxindoles as well as 4- and 5-alkenyloxindoles that inhibit or modulate protein kinases, in particular JNK protein kinases. The compounds of the invention and their pharmaceutically acceptable salts, and prodrugs of said compounds, are useful as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing the foregoing compounds, methods for the treatment and/or control of inflammation, particularly in the treatment or control of rheumatoid arthritis using these compounds, as well as intermediates useful in the preparation of compounds of the invention.
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