- TRICYCLIC INHIBITORS OF THE BCL6 BTB DOMAIN PROTEIN-PROTEIN INTERACTION AND USES THEREOF
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The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.
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- INHIBITORS OF THE BCL6 BTB DOMAIN PROTEIN-PROTEIN INTERACTION AND USES THEREOF
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The present application relates to compounds of Formula I (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.
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- Polyfluorinated salicylic acid derivatives as analogs of known drugs: Synthesis, molecular docking and biological evaluation
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We have developed the convenient methods for synthesis of polyfluorosalicylic acids and their derivatives. For the first time the biological properties of polyfluorosalicylates were investigated in vitro (permeability through the biological membranes, COX-1 inhibitory action) and in vivo (anti-inflammatory, analgesic activities, acute toxicity). Molecular docking of polyfluorinated salicylates confirmed in vitro and in vivo experiments.
- Shchegol'kov,Trefilova,Borisevich,Shchur,Ljushina,Khursan,Burgart, Ya.V.,Solodnikov, S.Yu.,Saloutin,Markova,Maslova,Krasnykh
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- A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity
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We have developed the practical method for polyfluorosalicylic acids synthesis via nucleophilic ortho-mono-substitution of fluorine atom with magnesium methoxide. We have managed to increase the yield of targeted polyfluorosalicylic acids from good to quantitative. We have studied the tuberculostatic activity of polyfluorosalicylic acids. It has been found that minimum inhibitory concentration (MIC) of compounds is from 0.7 to 6.5 μg/mL depending on the structure.
- Shchegol'Kov, Evgeny V.,Shchur, Irina V.,Burgart, Yanina V.,Saloutin, Victor I.,Solodnikov, Sergey Yu.,Krasnykh, Olga P.,Kravchenko, Marionella A.
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p. 2455 - 2458
(2016/07/07)
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- Design, synthesis and anticancer activity of functionalized spiro-quinolines with barbituric and thiobarbituric acids
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A new series of spiro-quinoline compounds have been accomplished by the reaction of barbituric acid or thiobarbituric acid with derivatives of benzisoxazole-5-carbaldehyde or 2-substituted benzaldehyde. These compounds were evaluated for their in vitro cy
- Bhaskarachar, Ravi Kiran,Revanasiddappa, Vijayakumar G.,Hegde, Subramanya,Balakrishna, Janardhana P.,Reddy, Suman Y.
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p. 3516 - 3528
(2015/08/03)
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- The regioexhaustive functionalization of difluorophenols and trifluorophenols through organometallic intermediates
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2,4-Difluorophenol, 2,5-difluorophenol, 2,3-difluorophenol, 3,5-difluorophenol, 3,4-difluorophenol, 2,4,5-trifluorophenol and 2,3,4-trifluorophenol were converted into all 18 possible di- or trifluorinated hydroxybenzoic acids (1a-c, 4a-c, 9a-c, 12a,b, 14a-c, 17a,b, 18a,b), all of them new compounds. The phenolic hydrogen atom was replaced by a methoxymethyl or, less frequently, by a triisopropylsilyl group, which exerted an ortho activating or ortho shielding effect, respectively. Sites flanked by two electronegative substituents (fluorine, alkoxy) were deprotonated with particular ease. They had to be silenced by the reversible attachment of a metalation-blocking trimethylsilyl group or of a metalation-deflecting chlorine atom if the metal was to be introduced elsewhere. In all cases but one, the stage was thus set for an intramolecular competition between metalation at an oxygen-adjacent or a fluorine-adjacent site. It proved indeed possible to secure the desired regioflexibility in either way by relying on an appropriate substrate-reagent matching. This demonstrates once more the potential of the organometallic approach to diversity-oriented synthesis.
- Marzi, Elena,Gorecka, Joanna,Schlosser, Manfred
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p. 1609 - 1618
(2007/10/03)
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- Regio-selective hydroxysubstitution of fluorobenzoic acid derivatives: Facile synthesis of fluorosalicylic acid derivatives
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Ortho-substituted fluorine in 2,4-difluorobenzoic acid was found to be regio-selectively replaced to hydroxide by solid sodium hydroxide in 1,3-dimethyl-2-imidazolidinone, to afford 4-fluoro-2-hydroxybenzoic acid in high yield. Several multi-fluoro-substi
- Umezu, Kazuto,Tabuchi, Fumiya,Kimura, Yoshikazu
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- 4-fluorosalicyclic acid derivative and process for production thereof
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PCT No. PCT/JP97/03761 Sec. 371 Date Jun. 12, 1998 Sec. 102(e) Date Jun. 12, 1998 PCT Filed Oct. 17, 1997 PCT Pub. No. WO98/17620 PCT Pub. Date Apr. 30, 1998The present invention provides a 4-fluorosalicylic acid derivative represented by the following ge
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