Total 18 PFD derivatives with the amide group replacing 5-methyl were synthesized and evaluated. YZQ17 possessed considerable antifibrosis activity in vitro via TGF-β/Smad2/3 pathway and was regarded as a lead compound for further optimization.
S2727 (Dacomitinib) was virtually screened out from a compound library via targeting the PC 190723 binding site of FtsZ and its inhibition effect on the functions of FtsZ was demonstrated by biological assays.
2-deoxystreptamine (2-DOS) conjugates with artificial nucleobases were designed and synthesized to inhibit pre-miR-372 processing into oncogenic miRNA and were discovered to be promising inhibitors when compared to their neomycin counterpart.
EED inhibitors to disable the PRC2 function were summarized.
Pharmacokinetic optimisation of the clinical candidate HBV capsid inhibitor AB-506 resulted in dramatic improvements in oral exposure and half-life providing compound 17 which demonstrated low dose QD efficacy in a mouse model of HBV replication.