Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.04.006
Abstract: A series of diverse small molecules have been designed and synthesized through structure-based drug design by taking advantage of fragment merging and elaboration approaches. Compounds ZL0420 (28) and ZL0454 (35) were identified as potent and… read more here.
Keywords: potent selective; brd4 inhibitors; airway inflammation; brd4 ... See more keywords
Design and Synthesis of Dual EZH2/BRD4 Inhibitors to Target Solid Tumors.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01876
Abstract: EZH2 inhibitors that prevent trimethylation of histone lysine 27 (H3K27) are often limited to the treatment of a subset of hematological malignancies. In most solid tumors, EZH2 inhibitors induce reciprocal H3K27 acetylation that subsequently results… read more here.
Keywords: design synthesis; ezh2; ezh2 brd4; brd4 inhibitors ... See more keywords