Ontology highlight
ABSTRACT:
SUBMITTER: Baud MG
PROVIDER: S-EPMC4770307 | biostudies-literature | 2016 Feb
REPOSITORIES: biostudies-literature
Baud Matthias G J MG Lin-Shiao Enrique E Zengerle Michael M Tallant Cynthia C Ciulli Alessio A
Journal of medicinal chemistry 20151001 4
We describe new synthetic routes developed toward a range of substituted analogues of bromo and extra-terminal (BET) bromodomain inhibitors I-BET762/JQ1 based on the triazolo-benzodiazepine scaffold. These new routes allow for the derivatization of the methoxyphenyl and chlorophenyl rings, in addition to the diazepine ternary center and the side chain methylene moiety. Substitution at the level of the side chain methylene afforded compounds targeting specifically and potently engineered BET brom ...[more]