Title : Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.

Pub. Date : 2015 Mar 1

PMID : 25678016






4 Functional Relationships(s)
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1 Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors. N6-benzoyladenine bromodomain containing 4 Homo sapiens
2 As a part of our continuing structural development studies of thalidomide to obtain a broad spectrum of biological modifiers based on the "multi-template" approach, in this work we focused on BRD4-inhibitory activity, and discovered that N6-benzoyladenine derivatives exhibit this activity. N6-benzoyladenine bromodomain containing 4 Homo sapiens
3 Structure-activity relationship studies led to N6-(2,4,5-trimethoxybenzoyl)adenine (29), which exhibits potent BRD4 bromodomain1 inhibitory activity with an IC50 value of 0.427muM. n6-(2,4,5-trimethoxybenzoyl)adenine bromodomain containing 4 Homo sapiens
4 N6-Benzoyladenine appears to be a new chemical scaffold for development of BRD4 inhibitors. N6-benzoyladenine bromodomain containing 4 Homo sapiens