4926-26-5Relevant articles and documents
QUINOLINE DERIVATIVES AS SMO INHIBITORS
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Paragraph 0512; 0513, (2017/02/28)
Disclosed are quinoline derivatives as hedgehog pathway inhibitors, especially as SMO inhibitors. Compounds of the present invention can be used in treating diseases relating to hedgehog pathway including cancer.
Exploring the influence of the protein environment on metal-binding pharmacophores
Martin, David P.,Blachly, Patrick G.,McCammon, J. Andrew,Cohen, Seth M.
supporting information, p. 7126 - 7135 (2014/11/07)
The binding of a series of metal-binding pharmacophores (MBPs) related to the ligand 1-hydroxypyridine-2-(1H)-thione (1,2-HOPTO) in the active site of human carbonic anhydrase II (hCAII) has been investigated. The presence and/or position of a single methyl substituent drastically alters inhibitor potency and can result in coordination modes not observed in small-molecule model complexes. It is shown that this unexpected binding mode is the result of a steric clash between the methyl group and a highly ordered water network in the active site that is further stabilized by the formation of a hydrogen bond and favorable hydrophobic contacts. The affinity of MBPs is dependent on a large number of factors including donor atom identity, orientation, electrostatics, and van der Waals interactions. These results suggest that metal coordination by metalloenzyme inhibitors is a malleable interaction and that it is thus more appropriate to consider the metal-binding motif of these inhibitors as a pharmacophore rather than a "chelator". The rational design of inhibitors targeting metalloenzymes will benefit greatly from a deeper understanding of the interplay between the variety of forces governing the binding of MBPs to active site metal ions.
Regio- and stereoselective syntheses of the natural product CCR5 antagonist anibamine and its three olefin isomers
Zhang, Feng,Zaidi, Saheem,Haney, Kendra M.,Kellogg, Glen E.,Zhang, Yan
experimental part, p. 7945 - 7952 (2011/11/30)
The syntheses of the natural product anibamine and its three olefin isomers have been achieved concisely and efficiently via highly regio- and stereoselective reactions. The crucial steps included a regioselective palladium-catalyzed alkynylation by Sonogashira coupling and a stereoselective Suzuki coupling. Further conformation analyses and in vitro calcium mobilization studies were carried out to characterize the compounds' biological properties.
LINEAR PYRIDAZINE AND PYRROLE COMPOUNDS, METHOD FOR OBTAINING THEM AND APPLICATIONS
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Page/Page column 33, (2010/02/16)
The present invention relates to linear pyridazine compounds, and more particularly to those of these compounds which are oligopyridazine compounds, to processes for obtaining them, to their uses, and also to their reduction to pyrroles and to the uses of the pyrrole, pyridazinylpyrrole and oligopyrrole compounds obtained. The invention relates in particular to the uses as medicaments, in particular for treating pathologies such as cancer, bacterial infections or parasitic infections, and also the applications in the materials, environmental, electronics and optics field.
2-(1H-INDAZOL-6-YLAMINO)-BENZAMIDE COMPOUNDS AS PROTEIN KINASES INHIBITORS USEFUL FOR THE TREATMENT OF OPHTALMIC DISEASES
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Page 50, (2010/02/07)
Indazole compounds that modulate and/or inhibit the ophthalmic diseases and the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating ophthalmic diseases and cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma,rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
New 2,2'-Bipyridine Derivatives and Their Luminescence Properties with Europium(III) and Terbium(III) Ions
Mukkala, Veli-Matti,Kankare, Jouko J.
, p. 1578 - 1592 (2007/10/02)
Twenty differently substituted 2,2',2",2"'-III and TbIII ions.The relative luminescence yields, excitation maxima, and emission decay constants were determined for the corresponding EuIII and TbIII chelates.The substituents at the bipyridine moiety had a significant effect on the luminescence properties: the best relative luminescence yields R were obtained for ligands with electron-donating substituents (e.g.Me, Ph), electron-withdrawing substituents (e.g.NO2, COOH) had a reverse effect.However, no clear correlation between the relative luminescence yields and the substituent parameters was found.