1. Diversity-oriented synthesis of marine sponge derived hyrtioreticulins and their anti-inflammatory activities
- Author
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LI Xu-wen, Guo Yue-Wei, Pang Tao, Liu Jin, Chen Bo-Ru, Gao Cheng-Long, and Jiang Jian-Lan
- Subjects
Drug ,medicine.drug_class ,media_common.quotation_subject ,medicine.medical_treatment ,Anti-Inflammatory Agents ,Anti-inflammatory ,Indole Alkaloids ,Structure-Activity Relationship ,Drug Discovery ,medicine ,Animals ,media_common ,Indole test ,Biological Products ,Pictet–Spengler reaction ,Indole alkaloid ,biology ,Chemistry ,Biological activity ,General Medicine ,biology.organism_classification ,Porifera ,Sponge ,Cytokine ,Complementary and alternative medicine ,Biochemistry - Abstract
Diversity-oriented synthesis is aiming to increase the chemical diversity of the 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 via 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 inhibitory rate of 92% at a concentration of 20 μM. A preliminary structure-activity relationship analysis was also discussed. This research may give an insight for the discovery of marine indole alkaloid derived anti-inflammatory drug leads.
- Published
- 2021