Discovery of the First BRD4 Second Bromodomain (BD2)-Selective Inhibitors.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c02516
Abstract: Pan-BD2 inhibitors have been shown to retain an antileukemia effect and display less dose-limiting toxicities than pan-BET inhibitors. However, it is necessary to consider the potential off-target toxicity associated with the inhibition of four BET… read more here.
Keywords: bd2; brd4 bd2; first brd4; selectivity ... See more keywords
Discovery of 2-(Pyrazol-4-yl)-quinazolin-4(3H)-one Derivatives as Subnanomolar BRD4 BD2 Inhibitors with High Selectivity via a Bioisosterism Approach.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c00924
Abstract: BRD4, a bromodomain-containing protein, has emerged as an attractive therapeutic target for various diseases. Selective inhibition of the bromodomain is gaining traction as a promising strategy for targeted drug discovery. Based on bioisosterism-guided optimization of… read more here.
Keywords: brd4 bd2; one derivatives; pyrazol quinazolin; quinazolin one ... See more keywords