On May 31, 2019, Gobbi, Silvia; Hu, Qingzhong; Foschi, Giacomo; Catanzaro, Elena; Belluti, Federica; Rampa, Angela; Fimognari, Carmela; Hartmann, Rolf W.; Bisi, Alessandra published an article.Application In Synthesis of 1-Fluoro-2-methoxybenzene The title of the article was Benzophenones as xanthone-open model CYP11B1 inhibitors potentially useful for promoting wound healing. And the article contained the following:
The inhibition of steroidogenic cytochrome P 450 enzymes has been shown to play a central role in the management of life-threatening diseases such as cancer, and indeed potent inhibitors of CYP19 (aromatase) and CYP17 (17伪 hydroxylase/17,20 lyase) are currently used for the treatment of breast, ovarian and prostate cancer. In the last few decades CYP11B1 (11-尾-hydroxylase) and CYP11B2 (aldosterone synthase), key enzymes in the biosynthesis of cortisol and aldosterone, resp., have been also investigated as targets for the identification of new potent and selective agents for the treatment of Cushing’s syndrome, impaired wound healing and cardiovascular diseases. In an effort to improve activity and synthetic feasibility of our different series of xanthone-based CYP11B1 and CYP11B2 inhibitors, a small series of imidazolylmethylbenzophenone-based compounds, previously reported as CYP19 inhibitors, was also tested on these new targets, in order to explore the role of a more flexible scaffold for the inhibition of CYP11B1 and -B2 isoforms. Compound 3 proved to be very potent and selective towards CYP11B1, and was thus selected for further optimization via appropriate decoration of the scaffold, leading to new potent 4′-substituted derivatives In this second series, 4 and 8, carrying a methoxy group and a Ph ring, resp., proved to be low-nanomolar inhibitors of CYP11B1, despite a slight decrease in selectivity against CYP11B2. Moreover, unlike the benzophenones of the first series, the 4′-substituted derivatives also proved to be selective for CYP11B enzymes, showing very weak inhibition of CYP19 and CYP17. Notably, the promising result of a preliminary scratch test performed on compound 8 confirmed the potential of this compound as a wound-healing promoter. The experimental process involved the reaction of 1-Fluoro-2-methoxybenzene(cas: 321-28-8).Application In Synthesis of 1-Fluoro-2-methoxybenzene
The Article related to benzophenone cyp11b1 cyp11b2 inhibitor wound healing cortisol steroidogenesis, benzophenone, cyp11b1 (11-尾-hydroxylase), cyp11b2 (aldosterone synthase), cortisol, steroidogenesis, wound healing and other aspects.Application In Synthesis of 1-Fluoro-2-methoxybenzene
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