Synthesis and biological evaluation of 2,3'-diindolylmethanes as agonists of aryl hydrocarbon receptor

2,3'-二吲哚甲烷作为芳烃受体激动剂的合成及生物学评价

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Abstract

Recent studies suggest that arylhydrocarbon receptor (AhR) may be a target for a number of diseases. Natural product malassezin is a AhR agonist with an interesting 2,3'-diindolylmethane skeleton. We have prepared a series of analogues of natural product malassezin using our recently developed method and tested the activity of these analogues against AhR in a cell-based assay. We found that a methyl substituent at 1'-N can significantly increase the activity and the 2-formyl group is not critical for some diindolylmethanes.

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