Design and Synthesis of 2,2'-Diindolylmethanes to Selectively Target Certain G-Quadruplex DNA Structures.

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Livendahl M, Jamroskovic J, Ivanova S, Demirel P, Sabouri N, Chorell E

Chemistry 22 (37) 13004-13009 [2016-09-05; online 2016-07-20]

G-quadruplex (G4) structures carry vital biological functions, and compounds that selectively target certain G4 structures have both therapeutic potential and value as research tools. Along this line, 2,2'-diindolylmethanes have been designed and synthesized in this work based on the condensation of 3,6- or 3,7-disubstituted indoles with aldehydes. The developed class of compounds efficiently stabilizes G4 structures without inducing conformational changes in such structures. Furthermore, the 2,2'-diindolylmethanes target certain G4 structures more efficiently than others and this G4 selectivity can be altered by chemical modifications of the compounds.

Chemical Biology Consortium Sweden (CBCS) [Collaborative]

PubMed 27431593

DOI 10.1002/chem.201602416

Crossref 10.1002/chem.201602416

Laboratories for Chemical Biology Umeå (LCBU)