Beilstein J. Org. Chem.2021,17, 1464–1475, doi:10.3762/bjoc.17.102
, and scalability to obtain gram amounts for biological studies. Selected compounds were found to display affinity for cannabinoidreceptors, which are promising drug targets for the treatment of inflammatory and neurodegenerative diseases.
Keywords: alkylation of indole; anti-inflammatory; binding
affinity; cannabinoidreceptors; diindolylmethane; unsymmetrical 3,3'-diindolylmethane; Introduction
Diindolylmethanes (DIMs) represent an important class of indole alkaloids, that are constituents of pharmaceuticals [1][2][3][4][5][6][7] and agrochemicals [8][9]. DIM derivatives possess a variety of
previously reported to bind to the cannabinoidreceptors, CB1 (Ki 4.3 µM) and CB2 (Ki 1.1 µM) [41]. Both receptors are considered important therapeutic targets, e.g. for neurodegenerative and inflammatory diseases. Selected final products (3a, 3b, 3e, 3g, 3h, 3n, 3ad) were tested for their binding affinities
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Graphical Abstract
Figure 1:
Diindolylmethanes and reported biological activities.