91813-07-9Relevant academic research and scientific papers
Synthesis, biological evaluation, and structure-activity relationships of novel substituted N-phenyl ureidobenzenesulfonate derivatives blocking cell cycle progression in s-phase and inducing DNA double-strand breaks
Turcotte, Vanessa,Fortin, Sébastien,Vevey, Florence,Coulombe, Yan,Lacroix, Jacques,C?té, Marie-France,Masson, Jean-Yves,C.-Gaudreault, René
experimental part, p. 6194 - 6208 (2012/08/27)
Twenty-eight new substituted N-phenyl ureidobenzenesulfonate (PUB-SO) and 18 N-phenylureidobenzenesulfonamide (PUB-SA) derivatives were prepared. Several PUB-SOs exhibited antiproliferative activity at the micromolar level against the HT-29, M21, and MCF-
ALKYLUREA DERIVATIVES ACTIVE AGAINST CANCER CELLS
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Page/Page column 24; 46, (2012/11/07)
Compounds of formula (I) : wherein A, m, n, R1, X, Y, R2, R3, R4, R5 and R6, as defined herein are provided as useful for the treatment of cancer or for the manufacture of anti-cancer agents.
SUBSTITUTED 2-IMIDAZOLIDONES AND ANALOGS
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Page/Page column 38, (2011/09/19)
Compounds of formula (I): wherein R1, R2, R3, R4, R7, R6, R7, R8, R9, A, X and Y as defined herein are provided as useful for the treatment of cancer or for
Design, synthesis, and structure-activity relationships of novel insulin receptor tyrosine kinase activators
Lum, Robert T.,Cheng, Mingshan,Cristobal, Cristina P.,Goldfine, Ira D.,Evans, Joseph L.,Keck, James G.,Macsata, Robert W.,Manchem, Vara Prasad,Matsumoto, Yukiharu,Park, Sophia J.,Rao, Sandhya S.,Robinson, Louise,Shi, Songyuan,Spevak, Wayne R.,Schow, Steven R.
scheme or table, p. 6173 - 6187 (2009/10/09)
A novel series of symmetrical ureas of [(7-amino(2-naphthyl))sulfonyl] phenylamines were designed, synthesized, and tested for their ability to increase glucose transport in mouse 3T3-L1 adipocytes, a surrogate readout for activation of the insulin receptor (IR) tyrosine kinase (IRTK). A structure-activity relationship was established that indicated glucose transport activity was dependent on the presence of two acidic functionalities, two sulfonamide linkages, and a central urea or 2-imidazolidinone core. Compound 30 was identified as a potent and selective IRTK activator. At low concentrations, 30 was able to increase the tyrosine phosphorylation of the IR stimulated by submaximal insulin. At higher concentrations, 30 was able to increase tyrosine the phosphorylation levels of the IR in the absence of insulin. When administered intraperitoneally (ip) and orally (po), 30 improved glucose tolerance in hypoinsulinemic, streptozotocin-treated rats. These data provide pharmacological validation that small molecule IRTK activators represent a potential new class of antidiabetic agents.
