832-53-1Relevant articles and documents
Development of HDAC Inhibitors Exhibiting Therapeutic Potential in T-Cell Prolymphocytic Leukemia
Toutah, Krimo,Nawar, Nabanita,Timonen, Sanna,Sorger, Helena,Raouf, Yasir S.,Bukhari, Shazreh,von Jan, Jana,Ianevski, Aleksandr,Gawel, Justyna M.,Olaoye, Olasunkanmi O.,Geletu, Mulu,Abdeldayem, Ayah,Israelian, Johan,Radu, Tudor B.,Sedighi, Abootaleb,Bhatti, Muzaffar N.,Hassan, Muhammad Murtaza,Manaswiyoungkul, Pimyupa,Shouksmith, Andrew E.,Neubauer, Heidi A.,de Araujo, Elvin D.,Aittokallio, Tero,Kr?mer, Oliver H.,Moriggl, Richard,Mustjoki, Satu,Herling, Marco,Gunning, Patrick T.
, p. 8486 - 8509 (2021/06/30)
Epigenetic targeting has emerged as an efficacious therapy for hematological cancers. The rare and incurable T-cell prolymphocytic leukemia (T-PLL) is known for its aggressive clinical course. Current epigenetic agents such as histone deacetylase (HDAC) inhibitors are increasingly used for targeted therapy. Through a structure-activity relationship (SAR) study, we developed an HDAC6 inhibitor KT-531, which exhibited higher potency in T-PLL compared to other hematological cancers. KT-531 displayed strong HDAC6 inhibitory potency and selectivity, on-target biological activity, and a safe therapeutic window in nontransformed cell lines. In primary T-PLL patient cells, whereHDAC6was found to be overexpressed, KT-531 exhibited strong biological responses, and safety in healthy donor samples. Notably, combination studies in T-PLL patient samples demonstrated KT-531 synergizes with approved cancer drugs, bendamustine, idasanutlin, and venetoclax. Our work suggests HDAC inhibition in T-PLL could afford sufficient therapeutic windows to achieve durable remission either as stand-alone or in combination with targeted drugs.
Polymer electrolyte and process for producing the same
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, (2008/06/13)
A polymer electrolyte having, in a main chain, a structural unit represented by the following formula (1):-[Ar1-(SO2-N-(X+)-SO2-Ar2)m-SO2-N-(X+)-SO2-Ar1-O]- wherein Ar1 and Ar2 independently represent a divalent aromatic groups, m represents an integer of 0 to 3, and X+ represents an ion selected from hydrogen ion, an alkali metal ion and ammonium ion, which is excellent in proton conductivity, thermal resistance and strength. The polymer electrolyte is soluble in solvents and has excellent film forming property and recycling efficiency.
Perfluoro- and Polyfluoro-sulphonic Acids. Part 22. Polyfluorophenyl Pentafluorobenzenesulphonates and their Electron Transfer Reaction with Sodium Iodide
Chen, Qing-Yun,Chen, Ming-Fang
, p. 1071 - 1075 (2007/10/02)
Polyfluorophenyl pentafluorobenzenesulphonates (1) have been synthesized in excellent yields by the reaction of pentafluorobenzenesulphonyl chloride with polyfluorophenoxides.Nucleophilic attack on 1 resulted in the breakage of the S-O bond accompanied by displacement of o- and /or p-fluorine.Reaction of 1 with sodium iodide (8) in a mole ratio of 1:3 (1:8) yielded polyfluorodiphenyl ethers 9 and 10 as the main products.However, p-C6F5OC6F4SO3C6F5 (12) was isolated as the major product in addition to 9 and 10 when the reactant ratio was 1:1 or 1:0.25.Reaction of 12 with sodium iodide also gave 9 and 10 when the reactant ratio was 1:3 (12:8).The reaction of 1 (or 12) with NaI is supposed to be an electron-transfer process.
STUDIEN ZUM VORGANG DER WASSERSTOFFUEBERTRAGUNG.61. Chemische Reaktivitaet und Halbstufenpotential Vergleichende Versuche am Beispiel einiger Arylsulfonsaeurederivate
Horner, Leopold,Schmitt, Rolf-Erhard
, p. 189 - 212 (2007/10/02)
In arylsulfonyl halides, the half-wave potentials of the corresponding chlorides and fluorides differ by more than 1000 mV, the fluoride being more negative; the influence of para-substituents is small for the chlorides, large for the fluorides.In agreement with the half-wave potentials, arylsulfonyl chlorides are considerably more reactive chemically than the corresponding fluorides.The O-selectivity found for P(O)F compounds is not observed in arylsulfonyl fluorides.Studies of competitive ester formation using primary and secondary alcohols and various arylsulfonyl chlorides yielded no clear analogy to the half-wave potentials.The primary alcohol is always sulfonated in preference to the secondary alcohol, whether the hydroxy functions are present in different molecules or the same molecule.In the latter case, the secondary hydroxyl function is then attacked in a further step by a second, different, arylsulfonyl chloride, giving the compounds 4-8.The further electroreduction of these diesters may be carried out in high yields, giving selective fission of one ester linkage only (that with the more positive potential) provided the difference in the half-wave potentials of the different ester linkages is sufficiently large.In the electroreductive fission the monosulfinic acid and the corresponding alcohol are liberated (see table II).In the competition reaction between phenol and 1:1 mixtures of tosyl chloride (A) and p-carboxyethyl-benzenesulfonyl chloride (B), the chloride with the more positive potential (B), E1/2=72 mV reacts quicker by a factor of 2.5.In competitive Finkelstein reactions, the selectivity was 1:11 at a difference in half-wave potentials of 760 mV (table IV).Arylsulfonates with free secondary alcohol functions may be oxidized smoothly and in high yield to the corresponding ketone using Na2Cr2O7 (3), without effecting the sulfonate linkage.The alkali hydrolysis of n-hexyl para-substituted arylsulfonates follows the Hammett relation but shows a lesser selectivity than was observed in the electroreductive fission of the same esters at the required potentials.Tables VI, VII and VIII concentrate on the preparative importance of the potential-controlled electroreductive fission of aliphatic and aromatic arylsulfonates.The corresponding hydroxy compounds are liberated in yields of up to over 90percent: N-alkyl- and N-aryl arylsulfonamides give analogous results. (table IX)
