940911-03-5Relevant academic research and scientific papers
A heterometallic macrocycle as a redox-controlled molecular hinge
Schouwey, Clment,Papmeyer, Marcus,Scopelliti, Rosario,Severin, Kay
, p. 2252 - 2258 (2015)
The ability to modify the structure of nanoscopic assemblies in a controlled fashion is an important prerequisite for the creation of functional supramolecular systems. Here, we describe a heterometallic Pt2Cu2-macrocycle which behaves as a molecular hinge. A square-planar Pt(ii) complex with pendent 2-formylpyridine groups was synthesized and structurally characterized. Condensation of the complex with benzylamine followed by reaction with Cu(MeCN)4BF4 resulted in the formation of a rectangular Pt2Cu2-macrocycle. Upon chemical oxidation of the Cu centers, the macrocycle folds up to adopt a butterfly-like geometry in which the Pt centers approach each other. This process can be reversed by chemical reduction.
NOVEL COMPOUNDS AS INHIBITORS OF HISTONE DEACETYLASE 6 AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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, (2022/01/24)
The present invention relates to a new compound having an inhibitory activity of histone deacetylase 6 (HDAC6), stereoisomers thereof, pharmaceutically acceptable salts thereof, a use thereof in the preparation of a drug, a pharmaceutical composition comprising them, a prophylactic or therapeutic method corresponding, and a method of preparing a new derivative 1,3,4-oxadiazole triazol, a novel compound having selective HDAC6 inhibitory activity being represented by the following chemical formula I.
RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Paragraph 00330-00331, (2020/07/06)
Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.
Spin-dimer networks: Engineering tools to adjust the magnetic interactions in biradicals
Borozdina, Yulia B.,Mostovich, Evgeny A.,Cong, Pham Thanh,Postulka, Lars,Wolf, Bernd,Lang, Michael,Baumgarten, Martin
, p. 9053 - 9065 (2017/09/22)
Magneto-structural correlations in stable organic biradicals have been studied on the example of weakly exchange coupled models with nitronyl nitroxide and imino nitroxide spin-carrying entities. Here, heteroatom substituted 2,2′-diaza- and 3,3′-diaza-tolane bridged biradicals were compared with the hydrocarbon analogue, while a biphenyl model with its 2,2′-bipyridine counterpart. For a 3,3′-diazatolane bridge the torsional angle between the nitronyl nitroxides and the pyridyl rings increased heavily (~52-54°) leading to a smaller theoretical intra-dimer exchange coupling value. However, a very large antiferromagnetic coupling was obtained experimentally. This could be appropriately explained by the presence of dominating inter-dimer exchange between the molecules. For the bis(imino nitroxide) with tolane bridge a field induced ordered state between 1.8 to 4.3 T in AC-susceptibility measurements was observed. In terms of a Bose Einstein condensate (BEC) of triplons this phenomenon could be described as a magnetic field induced ordered phase with 3D character.
2-ARYLBENZOFURAN-7-FORMAMIDE COMPOUNDS, PREPARATION METHOD AND USE THEREOF
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Paragraph 0076; 0110; 0111; 0112, (2015/02/18)
Provided in the present invention are a 2-arylbenzofuran-7-formamide compound as shown in general formula I or a pharmacologically or physiologically acceptable salt thereof, a preparation method thereof and use thereof in preparing anti-tumour drugs, whe
The discovery of polo-like kinase 4 inhibitors: Design and optimization of spiro[cyclopropane-1,3′[3H]indol]-2′(1′H).ones as orally bioavailable antitumor agents
Sampson, Peter B.,Liu, Yong,Patel, Narendra Kumar,Feher, Miklos,Forrest, Bryan,Li, Sze-Wan,Edwards, Louise,Laufer, Radoslaw,Lang, Yunhui,Ban, Fuqiang,Awrey, Donald E.,Mao, Guodong,Plotnikova, Olga,Leung, Genie,Hodgson, Richard,Mason, Jacqueline,Wei, Xin,Kiarash, Reza,Green, Erin,Qiu, Wei,Chirgadze, Nickolay Y.,Mak, Tak W.,Pan, Guohua,Pauls, Henry W.
, p. 130 - 146 (2016/09/09)
Polo-like kinase 4 (PLK4), a unique member of the polo-like kinase family of serine-threonine kinases, is a master regulator of centriole duplication that is important for maintaining genome integrity. Overexpression of PLK4 is found in several human cancers and is linked with a predisposition to tumorigenesis. Previous efforts to identify potent and efficacious PLK4 inhibitors resulted in the discovery of (E)-3-((1H-indazol-6-yl)methylene)indolin-2-ones, which are superseded by the bioisosteric 2-(1H-indazol-6-yl)spiro[cyclopropane-1,3′-indolin]-2′-ones reported herein. Optimization of this new cyclopropane-linked series was based on a computational model of a PLK4 X-ray structure and SAR attained from the analogous alkenelinked series. The racemic cyclopropane-linked compounds showed PLK4 affinity and antiproliferative activity comparable to their alkene-linked congeners with improved physicochemical, ADME, and pharmacokinetic properties. Positive xenograft results from the MDA-MB-468 human breast cancer xenograft model for compound 18 support the investigation of PLK4 inhibitors as anticancer therapeutics. A PLK4 X-ray co-structure with racemate 18 revealed preferential binding of the 1R,2S enantiomer to the PLK4 kinase domain.
2-ARYLBENZOFURAN-7-FORMAMIDE COMPOUNDS, PREPARATION METHOD AND USE THEREOF
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Paragraph 0021; 0044, (2015/01/18)
Provided in the present invention are a 2-arylbenzofuran-7-formamide compound as shown in general formula I or a pharmacologically or physiologically acceptable salt thereof, a preparation method thereof and use thereof in preparing anti-tumour drugs, whe
HYDROXAMIC ACID DERIVATIVES AS GRAM-NEGATIVE ANTIBACTERIAL AGENTS
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Page/Page column 55-56, (2010/09/18)
The invention relates to chemical compounds of formula (IB): or a salt thereof. In some embodiments, the invention relates to inhibitors of UDP-3-0 — (R-S-hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC). In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein and their use in the prevention and/or treatment of Gram- negative bacterial infections.
KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
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Page/Page column 181, (2010/11/03)
The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.
