Modification of Fragment Synthesis for the Purpose of Diversification of Fragment Screening Library
Human bromodomains, such as BRD4,when dysregulated, have been linked to cancer and heart disease. The regulation of these bromodomains is therefore interesting for drug discovery efforts, though selecting for the regulation of specific bromodomains has proven to be a challenge. In order to diversify the library of possible ligand components for the eventual regulation of BRD4, progress was made towards the synthesis of a modified ligand scaffold that has shown affinity to one of the previously identified binding sites of BRD4. Future experimental exploration of the usefulness of this ligand scaffold for developing ligands to bind BRD4 will follow. Possibly abstraction of the ligand scaffold into derivatives could serve to further diversify the fragment screening library.