Diversity-oriented synthesis of marine sponge derived hyrtioreticulins and their anti-inflammatory activities / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
; (6): 74-80, 2022.
Article
in En
| WPRIM
| ID: wpr-929238
Responsible library:
WPRO
ABSTRACT
Diversity-oriented synthesis is aimed to increase the chemical diversity of target natural products for extensive biological activity evaluation. Indole ring is an important functional group in a large number of drugs and other biologically active agents, and indole-containing natural products have been frequently isolated from marine sources in recent years. In this paper, a series of indole-containing marine natural hyrtioreticulin derivatives, including 19 new ones, were designed, synthesized through a key Pictet-Spengler reaction, and evaluated for their inflammation related activity. Compound 13b displayed the most promising activity by inhibiting TNF-α cytokine release with an inhibitory rate of 92% at a concentration of 20 μmol·L-1. A preliminary structure-activity relationship analysis was also discussed. This research may throw light on the discovery of marine indole alkaloid derived anti-inflammatory drug leads.
Key words
Full text:
1
Index:
WPRIM
Main subject:
Porifera
/
Structure-Activity Relationship
/
Biological Products
/
Indole Alkaloids
/
Anti-Inflammatory Agents
Limits:
Animals
Language:
En
Journal:
Chinese Journal of Natural Medicines (English Ed.)
Year:
2022
Type:
Article