252972-45-5Relevant academic research and scientific papers
Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents
Bassetto, Marcella,Ferla, Salvatore,Giancotti, Gilda,Pertusati, Fabrizio,Westwell, Andrew D.,Brancale, Andrea,McGuigan, Christopher
, p. 1414 - 1420 (2017)
Prostate cancer is a major cause of male death worldwide and the identification of new efficient treatments is constantly needed. Different non-steroidal androgen receptor antagonists are approved also in the case of castration-resistant cancer forms. Using a rational approach and molecular modelling studies to modify the structure of antiandrogen drug bicalutamide, a new series of phenylsulfonyl-benzamide derivatives was designed and synthesised. Their antiproliferative activities were evaluated in four different human prostate cancer cell lines and several new compounds showed significantly improved IC50 values in the low μM range. The cytotoxicity profile was also evaluated for the novel structures in the HEK293 cell line.
NOVEL GLUCOCORTICOID RECEPTOR AGONISTS
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Page/Page column 37, (2010/12/26)
This invention relates to novel glucocorticoid receptor agonists of formula (I) and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to their combination with one or more other therapeutic agents, as well as to their use for the treatment of a number of inflammatory and allergic diseases, disorders and conditions.
Nitrophenyl derivatives as aldose reductase inhibitors
Costantino, Luca,Ferrari, Anna Maria,Gamberini, Maria Cristina,Rastelli, Giulio
, p. 3923 - 3931 (2007/10/03)
Nitrophenyl derivatives were recently discovered as a new class of ALR2 inhibitors by means of docking and database screening of the National Cancer Institute database of organic molecules. The nitro group was predicted to bind to the Tyr48 and His110 act
