- Synthesis of palladium complexes with quinolino-based tridentate ligands and their applications for norbornene polymerization
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Palladium complexes bearing new tridentate quinolino-based [N?NNox] ligands were synthesized and tested for the polymerization of norbornene. Upon activation of MAO, all the palladium complexes showed high catalytic activities for th
- Liu, Hui,Shi, Xiaochao,You, Fen,Yuan, Haibin
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- INHIBITORS OF RPN11
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Candidate compounds for specific inhibition of Rpn11 are represented by Formula 1a where each of R2, R3, R4, R5, R6, and R7 is independently selected from hydrogen (H), substituted and unsubstituted alkyl groups, carboxyl groups, or substituted and unsubstituted carboxyamides.
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Paragraph 0091
(2017/03/14)
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- Discovery of an Inhibitor of the Proteasome Subunit Rpn11
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The proteasome plays a crucial role in degradation of normal proteins that happen to be constitutively or inducibly unstable, and in this capacity it plays a regulatory role. Additionally, it degrades abnormal/damaged/mutant/misfolded proteins, which serves a quality-control function. Inhibitors of the proteasome have been validated in the treatment of multiple myeloma, with several FDA-approved therapeutics. Rpn11 is a Zn2+-dependent metalloisopeptidase that hydrolyzes ubiquitin from tagged proteins that are trafficked to the proteasome for degradation. A fragment-based drug discovery (FBDD) approach was utilized to identify fragments with activity against Rpn11. Screening of a library of metal-binding pharmacophores (MBPs) revealed that 8-thioquinoline (8TQ, IC50 value ~2.5 μM) displayed strong inhibition of Rpn11. Further synthetic elaboration of 8TQ yielded a small molecule compound (35, IC50 value ~400 nM) that is a potent and selective inhibitor of Rpn11 that blocks proliferation of tumor cells in culture.
- Perez, Christian,Li, Jing,Parlati, Francesco,Rouffet, Matthieu,Yuyong,Mackinnon, Andrew L.,Chou, Tsui-Fen,Deshaies, Raymond J.,Cohen, Seth M.
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p. 1343 - 1361
(2017/03/08)
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- Quinoline-derived two-photon sensitive quadrupolar probes
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The first quadrupolar 8-dimethylaminoquinoline-derived 6-(8-DMAQ-OAc)2 (1c) and 5-(8-DMAQ-OAc)2 (2c) photosensitive probes underwent photolysis under UV (365 nm) and NIR (730 nm two-photon (TP)) irradiation conditions, showing Q
- Dunkel, Petra,Tran, Christine,Gallavardin, Thibault,Dhimane, Hamid,Ogden, David,Dalko, Peter I.
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p. 9899 - 9908
(2015/01/08)
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- COMPOSITIONS AND METHODS FOR JAMM PROTEIN INHIBITION
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Compounds, pharmaceutical compositions, and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by JAMM proteins are disclosed.
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Page/Page column 90
(2014/05/24)
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- High throughput one pot synthesis of 2-methylquinolines
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Various 2-methylquinolines have been successfully synthesized by using anilines and ethyl vinyl ether in 1:3 mole ratios in the presence of acetic acid. Stirring at rt for 3-4 h followed by reflux for 3.5-4 h resulted in the corresponding 2-methylquinolines in good yield. Copyright
- Chandrashekarappa, Kiran Kumar H.,Mahadevan, Kittappa M.,Manjappa, Kiran B.
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p. 1368 - 1370
(2013/04/23)
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- QU1NOLINE DERIVATIVES AND THEIR USES FOR RHINITIS AND URTICARIA
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The present invention relates to compounds of formula (I) and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various diseases, such as allergic rhinitis.
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Page/Page column 42
(2010/09/17)
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- Novel N-acylated heterocycles
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Described are compositions comprising a muscarinic receptor antagonist and an N-acylated heterocycle derivative having affinity for serotonergic receptors, and enantiomers, diastereoisomers, N-oxides, polymorphs, solvates and pharmaceutically acceptable salts thereof. The combination of a muscarinic receptor antagonist and an N-acylated heterocycle, or an enantiomer, diastereoisomer, N-oxide, polymorph, solvate or pharmaceutically acceptable salt thereof, is useful in the treatment of patients with neuromuscular dysfunction of the lower urinary tract and diseases related to 5-HT1A receptors.
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- Preparation and evaluation of sulfur-containing metal chelators
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With a view to probe the structure and function of G-protein coupled receptors the synthesis of functionalized 8-mercaptoquinoline derivatives and 2-(2-pyridyl)thiophenol was achieved. A fluorescence-based method for determining the affinity of these metal chelators toward zinc ions was developed.
- Clavier, Sylvain,Rist, ystein,Hansen, Stina,Gerlach, Lars-Ole,Hoegberg, Thomas,Bergman, Jan
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p. 4248 - 4253
(2007/10/03)
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- Quinoline compound
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Compounds of formula I STR1 wherein R1 -R5, X, Ar and Y are as defined in the description, have valuable pharmaceutical properties and are especially effective as leukotriene antagonists. They are prepared in a manner known per se.
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