C-H chlorination of (hetero)anilines photo/organo co-catalysis.

Chlorinated (hetero)anilines are a class of important structural motifs that are widely present in synthetic building blocks and pharmaceuticals. Despite recent advancements, direct aniline chlorination still suffers from / and mono/poly chlorination selectivity problems. Herein, we disclose a photo-redox and organo co-catalyzed chlorination method for anilines.

Design and synthesis of dual inhibitors targeting snail and histone deacetylase for the treatment of solid tumour cancer.

Snail and histone deacetylases (HDACs) have an important impact on cancer treatment, especially for their synergy. Therefore, the development of inhibitors targeting both Snail and HDAC might be a promising strategy for the treatment of cancers. In this work, we synthesized a series of Snail/HDAC dual inhibitors.

Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model.

FLT3 mutation is among the most common genetic mutations in acute myeloid leukemia (AML), which is also related with poor overall survival and refractory in AML patients. Recently, FLT3 inhibitors have been approved for AML therapy. Herein, a series of new compounds with pyrazole amine scaffold was discovered, which showed potent inhibitory activity against FLT3-ITD and significant selectivity against both FLT3-ITD and AML cells expressing FLT3-ITD.