880139-06-0Relevant academic research and scientific papers
Synthesis, biological evaluation, and docking study of indole aryl sulfonamides as aromatase inhibitors
Fantacuzzi, Marialuigia,De Filippis, Barbara,Gallorini, Marialucia,Ammazzalorso, Alessandra,Giampietro, Letizia,Maccallini, Cristina,Aturki, Zeineb,Donati, Enrica,Ibrahim, Reham S.,Shawky, Eman,Cataldi, Amelia,Amoroso, Rosa
, (2020)
In order to identify new aromatase enzyme inhibitors, thirty aryl sulfonamide derivatives containing an indole nucleus have been synthesized. The enzyme inhibition assay showed that four compounds inhibit aromatase in the sub-micromolar range. Loading concentrations of these four compounds were afterwards tested for cell viability and cytotoxicity on MCF7 human breast cancer cells, revealing a time- and dose-dependent decrease of active metabolizing cells over the time of the culture (0–72 h), starting from a concentration of 100 μM. Likewise LDH released raised up to 40% at early time of exposures (24 h). Finally, the docking study showed that the best active compounds efficiently bound in the active site of the aromatase; high values of HBD and low levels of HBA are the principal requirement evidenced by the QSAR model.
Inhibitors of 15-lipoxygenase
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Page/Page column 15, (2008/06/13)
The present invention provides inhibitors of 15-LO according to Formula I, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions.
