- BTB-1 A small molecule inhibitor of the mitotic motor protein kif18A
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Turning the motor off: A malachite green based assay leads to the identification of BTB-1 (see picture), the first small-molecule inhibitor of the mitotic motor protein Kif18A. BTB-1 reversibly inhibits the ATPase activity of the recombinant motor domain
- Catarinella, Mario,Gruener, Tamara,Strittmatter, Tobias,Marx, Andreas,Mayer, Thomas U.
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Read Online
- Synthesis of thioethers, arenes and arylated benzoxazoles by transformation of the C(aryl)-C bond of aryl alcohols
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Transformation of aryl alcohols into high-value functionalized aromatic compounds by selective cleavage and functionalization of the C(aryl)-C(OH) bond is of crucial importance, but very challenging by far. Herein, for the first time, we report a novel and versatile strategy for activation and functionalization of C(aryl)-C(OH) bonds by the cooperation of oxygenation and decarboxylative functionalization. A diverse range of aryl alcohol substrates were employed as arylation reagents via the cleavage of C(aryl)-C(OH) bonds and effectively converted into corresponding thioether, arene, and arylated benzoxazole products in excellent yields, in a Cu based catalytic system using O2 as the oxidant. This study offers a new way for aryl alcohol conversion and potentially offers a new opportunity to produce high-value functionalized aromatics from renewable feedstocks such as lignin which features abundant C(aryl)-C(OH) bonds in its linkages.
- Chen, Bingfeng,Han, Buxing,Liu, Mingyang,Meng, Qinglei,Song, Jinliang,Zhang, Pei,Zhang, Zhanrong
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p. 7634 - 7640
(2020/08/14)
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- Quinazolinone and isoquinolinone derivative
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The present invention relates to quinazolinone and isoquinolinone derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
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Paragraph 0319; 0320
(2016/10/08)
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- Aerobic copper-catalyzed decarboxylative thiolation
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Copper-catalyzed decarboxylative thiolation using molecular oxygen as the sole oxidant was developed. A variety of aromatic carboxylic acids including 2-nitrobenzoic acids, pentafluorobenzoic acid and several heteroaromatic carboxylic acids undergo efficient thiolation to furnish the aryl sulfides in moderate to excellent yields.
- Li, Minghao,Hoover, Jessica M.
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supporting information
p. 8733 - 8736
(2016/07/15)
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- Modulation of cAMP-specific PDE without emetogenic activity: New sulfide-like PDE7 inhibitors
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A forward chemical genetic approach was followed to discover new targets and lead compounds for Parkinson's disease (PD) treatment. By analysis of the cell protection produced by some small molecules, a diphenyl sulfide compound was revealed to be a new phosphodiesterase 7 (PDE7) inhibitor and identified as a new hit. This result allows us to confirm the utility of PDE7 inhibitors as a potential pharmacological treatment of PD. On the basis of these data, a diverse family of diphenyl sulfides has been developed and pharmacologically evaluated in the present work. Moreover, to gain insight into the safety of PDE7 inhibitors for human chronic treatment, we evaluated the new compounds in a surrogate emesis model, showing nonemetic effects.
- García, Ana M.,Brea, José,Morales-García, Jose A.,Perez, Daniel I.,González, Alejandro,Alonso-Gil, Sandra,Gracia-Rubio, Irene,Ros-Simó, Clara,Conde, Santiago,Cadavid, María Isabel,Loza, María Isabel,Perez-Castillo, Ana,Valverde, Olga,Martinez, Ana,Gil, Carmen
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p. 8590 - 8607
(2014/12/11)
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- BENZOFURAN-2-SULFONAMIDES DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS
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The present invention relates to novel benzofuran-2-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
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Paragraph 0341; 0342; 0343
(2013/09/12)
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- Diaryl sulfide-based inhibitors of trypanothione reductase: Inhibition potency, revised binding mode and antiprotozoal activities
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Trypanothione reductase (TR) is an essential enzyme of trypanosomatids and therefore a promising target for the development of new drugs against African sleeping sickness and Chagas′ disease. Diaryl sulfides with a central anilino moiety, decorated with a
- Stump, Bernhard,Eberle, Christian,Kaiser, Marcel,Brun, Reto,Krauth-Siegel, R. Luise,Diederich, Francois
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scheme or table
p. 3935 - 3947
(2009/06/28)
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- Antitrypanosomal, antileishmanial, and antimalarial activities of quaternary arylalkylammonium 2-amino-4-chlorophenyl phenyl sulfides, a new class of trypanothione reductase inhibitor, and of N-acyl derivatives of 2-amino-4-chlorophenyl phenyl sulfide
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Quaternization of the nitrogen atom of 2-amino-4-chlorophenyl phenyl sulfide analogues of chlorpromazine improved inhibition ～40-fold (3′,4′-dichlorobenzyl-[5-chloro-2-phenylsulfanylphenylamino)-propyl] -dimethylammonium chloride inhibited trypanothione r
- Parveen, Seheli,Khan, Mohammed O. F.,Austin, Susan E.,Croft, Simon L.,Yardley, Vanessa,Rock, Peter,Douglas, Kenneth T.
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p. 8087 - 8097
(2007/10/03)
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- Electron ionization-induced loss of SO2 from 2-nitrodiaryl sulfides
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Electron ionization-induced loss of SO2 from 2-nitrodiphenyl sulfide leads to the same ionic structure, or mixture of structures, as loss of N2 from the molecular ion of N1-phenylbenzotriazole. Ab initio calculations are i
- Lambert,Bertin,Lacoste,Volland,Krick,Furet,Botrel,Guenot
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p. 242 - 249
(2007/10/03)
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- New spermine and spermidine derivatives as potent inhibitors of trypanosoma cruzi trypanothione reductase
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Several spermine and spermidine derivatives containing 2-amino diphenylsulfide substituents were prepared and tested for their inhibiting effects on Trypanosoma cruzi trypanothione reductase. IC50 values were assessed between 0.3 and 3 μM. Compound 32 (K(i) = 0.4 μM) is the most potent TR inhibitor described so far.
- Bonnet, Beatrice,Soullez, David,Davioud-Charvet, Elisabeth,Landry, Valerie,Horvath, Dragos,Sergheraert, Christian
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p. 1249 - 1256
(2007/10/03)
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- Substituted dibenzoxazepine and dibenzthiazepine carbamate compounds, pharmaceutical compositions and methods of use
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The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: STR1 which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a com
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- 1-,2-,3-,4-,5-,6-,7-,8- AND/OR 9 SUBSTITUTED DIBENZOXAZEPINE COMPOUDS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATING PAIN
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The present invention provides substituted dibenzoxazepine compounds of Formula I: STR1 which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
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- 2-, 3-, 4-, 5-, 6-, 7-, 8-, 9- and/or 10-substituted dibenzoxazepine and dibenzthiazepine compounds, pharmaceutical compositions and methods of use
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The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: STR1 which are useful as analgesic agents for the treatment of pain, and for prostaglandin-E2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal, and a method for treating prostaglandin-E2 mediated diseases in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
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- 8-substituted-dibenz[b,f][1,4]oxazepine-10(11)-carboxylic acid, substituted hydrazides, pharmaceutical compositions, and methods for treating pain
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The present invention provides substituted dibenzoxazepine compounds of Formula I: STR1 wherein X is STR2 which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
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