2. Academic Validation
  3. Design and Synthesis of Marine Phidianidine Derivatives as Potential Immunosuppressive Agents

Design and Synthesis of Marine Phidianidine Derivatives as Potential Immunosuppressive Agents

  • J Med Chem. 2018 Dec 27;61(24):11298-11308. doi: 10.1021/acs.jmedchem.8b01430.
Jin Liu 1 2,  Heng Li 2 3,  Kai-Xian Chen 1 4,  Jian-Ping Zuo 2 3,  Yue-Wei Guo 1 2 4,  Wei Tang 2 3 4,  Xu-Wen Li 1 2 4
Affiliations

Affiliations

  • 1 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica , Chinese Academy of Sciences , 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park , Shanghai 201203 , China.
  • 2 University of Chinese Academy of Sciences , No. 19A Yuquan Road , Beijing 100049 , China.
  • 3 Laboratory of Immunopharmacology, Shanghai Institute of Materia Medica , Chinese Academy of Sciences , Shanghai 201203 , China.
  • 4 Open Studio for Druggability Research of Marine Natural Products , Pilot National Laboratory for Marine Science and Technology (Qingdao) , 1 Wenhai Road , Aoshanwei, Jimo, Qingdao 266237 , China.
PMID: 30500185 DOI: 10.1021/acs.jmedchem.8b01430
Abstract

A series of novel marine phidianidine derivatives were designed, synthesized, and evaluated for their immunosuppressive activities during our search of potential immunosuppressive agents with high efficacy and low toxicity from marine sources. These compounds were tested for their inhibitory activity on Con A-induced T cell and lipopolysaccharide-induced B cell proliferation. Compounds 14a and 18c, displaying the most promising inhibitory effects and low toxicities, were further found to possess immune-regulatory activities upon cross-linking of T cell receptor (TCR) and B cell receptor (BCR) on purified T and B cells, respectively.

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