Synthesis, biological evaluation, and docking study of indole aryl sulfonamides as aromatase inhibitors was written by 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. And the article was included in European Journal of Medicinal Chemistry in 2020.Electric Literature of C8H9ClO4S This article mentions the following:
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 100μM. 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. In the experiment, the researchers used many compounds, for example, 2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2Electric Literature of C8H9ClO4S).
2,4-Dimethoxybenzene-1-sulfonyl chloride (cas: 63624-28-2) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations.While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.Electric Literature of C8H9ClO4S
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics