Background: Histone acetylation is an essential approach of post-translational modification
(PTM) and a significant component of epigenetic regulation that is mediated by Bromodomainscontaining
protein (BRDs). In recent years, many researchers have found that a variety of malignancy,
inflammatory and other diseases occurrences and developments are associated with BRD4 expression
disorders or dysfunction. Meanwhile, many inhibitors of the extra-terminal (BET) family have been
reported in many papers.
Objective: This review summarized those newly found BET inhibitors, their mechanism of action and
bioactivity. Secondly, those compounds were mainly classified based on their structures and their
structure-activity relationship information was discussed. Beyond that, every compound’s design
strategy was pointed out.
Results and Conclusion: Herein, the recent advances reported were reviewed for discovering more
excellent small molecule inhibitors. Currently, in addition to compound 4, compounds 7, 22 and 90,
have also been into the clinical trial stage. In the view of the outstanding performance of BET inhibitors
in anti-tumor, anti-inflammatory and anti-drug resistance, we believe that more and more BET inhibitors
will become the new epigenetic therapy for cancer, inflammation and autoimmune disease in
clinical practice in the near future.