100246-31-9Relevant academic research and scientific papers
Cyclizing radical carboiodination, carbotelluration, and carboaminoxylation of aryl amines
Hartmann, Marcel,Studer, Armido
supporting information, p. 8180 - 8183 (2014/08/18)
Radical carboiodination of various aryl amines is reported. Aryl diazonium salts, generated in situ from the corresponding aryl amines, are reacted with Bu4NI to provide the corresponding aryl radicals which undergo 5-exo or 6-exo cyclization. Iodine abstraction eventually affords the carboiodinated products in good to excellent yields. If TEMPO is added, the cascade provides the cyclized carboaminoxylation products. Running the reaction in the presence of PhTeTePh affords the phenyltellurated cyclized products.
Synthesis and in-vitro biological activity of macrocyclic urea Chk1 inhibitors
Li, Gaoquan,Tao, Zhi-Fu,Tong, Yunsong,Przytulinska, Magdalena K.,Kovar, Peter,Merta, Philip,Chen, Zehan,Zhang, Haiying,Sowin, Thomas,Rosenberg, Saul H.,Lin, Nan-Horng
, p. 6499 - 6504 (2008/03/18)
A variety of macrocyclic urea compounds were prepared as potent Chk1 inhibitors by modifying the C5 position of the benzene ring of the macrocyclic urea with ether moieties, aliphatic carbon chains, amide and halides. Enzymatic activity less than 20 nM was observed in 29 of 40 compounds. Compounds 14, 46d, and 48j provided the best overall results in the cellular assays as they abrogated doxorubicin-induced cell cycle arrest (IC50 = 3.31, 3.08, and 3.13 μM) and enhanced doxorubicin cytotoxicity (IC50 = 0.54, 1.27, and 0.96 μM) while displaying no single agent activity, respectively.
