Research progress on stimulator of interferon genes agonists for cancer immunotherapy / 中国药科大学学报

@#In recent years, tumor immunotherapy has become a new hot spot in the field of cancer treatment. Besides the great success of immunological checkpoint inhibitors and cellular immunotherapy, small molecule immunotherapy has also attracted more and more attention. As a key signal transduction molecule involved in the innate immune response, stimulator of interferon genes plays an important role in defending against viral and intracellular bacterial infections, mediating type I IFN production and regulating the production of spontaneous anti-tumor immune responses in vivo. This paper briefly introduces the biological mechanism of STING signaling pathway and reviews the research progress of STING agonists based on the structural classification, so as to provide some reference for the design and discovery of STING agonist drugs.

Total synthesis of cyclodepsipeptide Hikiamides A-C / 中国药科大学学报

@#Total synthesis of cyclodepsipeptide Hikiamides A-C was described. Fragment convergent condensation method was applied for the preparation of Hikiamides A-C, starting from Commercially available amino acid such as L-N-Boc-Phe-OH, L-N-Boc-Trp-OH, L-N-Cbz-Van-OH etc. Tripeptide fragments(compounds 5a/5b)and dipeptide fragments(compounds 8a/8b)were first prepared. The subsequent condensation of the resulted two fragments provided protected linear pentapetides(compounds 9a/9b/9c); Finally, the linear pentapetide was cyclized by a mixed condensing agents comprised of PyBOP and HBTU. Hikiamides A-C was obtained with total yields of 9%, 11% and 6. 5%, respectively. Compared with the natural source, this method has the advantages of low cost, convenient operation and high yield, which effectively solves the problem of low isolated yield of Hikiamides A-C from Fusarium sp.

Total synthesis of sauropunol A-D isolated from Sauropus rostratus genus plants / 中国药科大学学报

Sauropunol A-D potentially with anti-inflammatory,anti-bacterial activities were recently isolated from traditional Chinese medicinal plant Sauropus rostratus.Herein,we report the total synthesis of sauropunol (A-D) starting from a commercially available 2-deoxy-D-arabino-hexopyranose.The trifluoromethane sulfonation of intermediates could simultaneously trigger intramolecular cyclization to afford 3,6-anhydro hexofuranoside scaffold.The following deprotection reaction could produce sauropunol A,B and C/D with total yields of 21％,5％,and 17％ (isomer sauropunol C/D),respectively.Structures of the target compounds were confirmed by comparison with NMR spectroscopic properties of those previously reported.