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.
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.
