Gu Yiming, Yu Wei, Li Xiang, Fan Yingjie, Liu Yanan, Tummatorn Jumreang, Jiang Siyu, Yang Jingyue
State Key Laboratory of Metastable Materials Science and Technology, Nano-biotechnology Key Lab of Hebei Province, Applying Chemistry Key Lab of Hebei Province, Yanshan University, Qinhuangdao, 066004, China.
Qinhuangdao Customs Technology Center, Qinhuangdao, Hebei, 066004, China.
ChemMedChem. 2025 May 5;20(9):e202400979. doi: 10.1002/cmdc.202400979. Epub 2025 Feb 17.
To address the metabolic instability of cordycepin induced by adenosine deaminase (ADA) and to enhance its bioactivity, this study developed eleven novel cordycepin derivatives using molecular engineering techniques. By incorporating sterically hindered protective groups and modifying the glycosyl moiety, the research aimed to improve both stability and efficacy. Antibacterial tests revealed that five derivatives showed significantly greater activity against pathogenic strains compared to cordycepin, with better compatibility with probiotics. Compound 2 c demonstrated moderate antitumor activity against K562 and MGC-803 cells, with IC values of 42.21 μM and 27.79 μM, respectively. Additionally, compound 4 b demonstrated notable DPPH free radical scavenging ability. These compounds also showed improved stability in ADA solutions, providing valuable insights into the structure-activity relationships of cordycepin derivatives.
