4548-56-5Relevant academic research and scientific papers
BTB-1 A small molecule inhibitor of the mitotic motor protein kif18A
Catarinella, Mario,Gruener, Tamara,Strittmatter, Tobias,Marx, Andreas,Mayer, Thomas U.
, p. 9072 - 9076 (2009)
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
Synthesis of thioethers, arenes and arylated benzoxazoles by transformation of the C(aryl)-C bond of aryl alcohols
Chen, Bingfeng,Han, Buxing,Liu, Mingyang,Meng, Qinglei,Song, Jinliang,Zhang, Pei,Zhang, Zhanrong
, p. 7634 - 7640 (2020/08/14)
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.
Quinazolinone and isoquinolinone derivative
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Paragraph 0280; 0322, (2016/10/08)
The present invention relates to quinazolinone and isoquinolinone derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
Aerobic copper-catalyzed decarboxylative thiolation
Li, Minghao,Hoover, Jessica M.
supporting information, p. 8733 - 8736 (2016/07/15)
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.
Modulation of cAMP-specific PDE without emetogenic activity: New sulfide-like PDE7 inhibitors
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
, p. 8590 - 8607 (2014/12/11)
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.
BENZOFURAN-2-SULFONAMIDES DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS
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Paragraph 0341; 0342; 0343, (2013/09/12)
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.
Diaryl sulfide-based inhibitors of trypanothione reductase: Inhibition potency, revised binding mode and antiprotozoal activities
Stump, Bernhard,Eberle, Christian,Kaiser, Marcel,Brun, Reto,Krauth-Siegel, R. Luise,Diederich, Francois
scheme or table, p. 3935 - 3947 (2009/06/28)
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
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
Parveen, Seheli,Khan, Mohammed O. F.,Austin, Susan E.,Croft, Simon L.,Yardley, Vanessa,Rock, Peter,Douglas, Kenneth T.
, p. 8087 - 8097 (2007/10/03)
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
Electron ionization-induced loss of SO2 from 2-nitrodiaryl sulfides
Lambert,Bertin,Lacoste,Volland,Krick,Furet,Botrel,Guenot
, p. 242 - 249 (2007/10/03)
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
New spermine and spermidine derivatives as potent inhibitors of trypanosoma cruzi trypanothione reductase
Bonnet, Beatrice,Soullez, David,Davioud-Charvet, Elisabeth,Landry, Valerie,Horvath, Dragos,Sergheraert, Christian
, p. 1249 - 1256 (2007/10/03)
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.
