Non-steroidal aromatase inhibitors based on a biphenyl scaffold: synthesis, in vitro SAR, and molecular modelling was written by Jackson, Toby;Woo, L. W. Lawrence;Trusselle, Melanie N.;Purohit, Atul;Reed, Michael J.;Potter, Barry V. L.. And the article was included in ChemMedChem in 2008.Electric Literature of C7H6BrF This article mentions the following:
The synthesis and in vitro biol. evaluation (JEG-3 cells) of a series of novel and potent aromatase inhibitors, prepared by microwave-enhanced Suzuki cross-coupling methodol., are reported. These compounds possess a biphenyl template incorporated with the haem-ligating triazolylmethyl moiety, either on its own or in combination with other substituent(s) at various positions on the Ph rings. The most potent aromatase inhibitor reported herein has an IC50 value of 0.12 nM, although seven of its congeners are also highly potent (IC50 閳?0.5 nM). They all bear the (5-triazolylmethyl-2-cyano)biphenyl structural motif. Docking of representative compounds into a homol. model of human aromatase assists in the rationalisation of the SAR derived from the in vitro biol. results and supports a crucial role for a cyano group on the “A” Ph ring, which is accessible to hydrogen bond interactions with Ser478. Further development of these compounds as potential therapeutic agents for the treatment of hormone-dependent breast cancer is warranted given the high level of potency observed for this class of aromatase inhibitor in vitro. In the experiment, the researchers used many compounds, for example, 3-Bromo-4-fluorotoluene (cas: 452-62-0Electric Literature of C7H6BrF).
3-Bromo-4-fluorotoluene (cas: 452-62-0) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon鑱砨romine bond is electrophilic in nature. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Electric Literature of C7H6BrF
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary