“…1 ), which demonstrated efficacy and safety in phase II trials as an anti-migraine agent. 1,2 In addition, DHQs with potent anti-HIV, 3 anti-psychotic, 4,5 anti-cancer 6,7 and anti-microbial 8 activities as well as potential for the treatment of cardiovascular 9 and anti-inflammatory disorders 10 have been disclosed. Recently PFI-1, a potent and selective inhibitor of the bromo- and extra C-terminal domain (BET) family of bromodomains was developed using a fragment based approach starting from small DHQ-containing hit.…”