1. Total Synthesis and Anti-HIV Activity Evaluation of Desmosdumotin D and Analogues
- Author
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Ying Deng, Xiaoping Song, Tongtong Yun, Zuo Xiang, Guanghui Wang, Gang Li, Yanxin Zhang, Yiming Song, and Qingchao Liu
- Subjects
Desmosdumotin D ,chemical synthesis ,analogue ,HIV-1 ,Pharmacy and materia medica ,RS1-441 ,Chemistry ,QD1-999 - Abstract
The natural product Desmosdumotin D (hereafter referred to as Des-D), isolated from the plant Desmos dumosus, showed potent anti-HIV activity. However, the subsequent pharmacological activity and clinical studies are limited due to the low content of Des-D in the plant. Therefore, the total synthesis path of Des-D was optimized in this paper, and the total yield was increased from 4.4% to 11.9%. Additionally, twelve analogues were obtained following the synthesis route of Des-D. The anti-HIV activity evaluation results in vitro showed that Des-D had the highest activity, with an IC50 value of 13.6 μM, and compounds 17 and 11 had the lowest anti-HIV activity, with IC50 values of 101.3 μM and 161.0 μM, respectively. Through the molecular docking of compounds Des-D and 17 with HIV-IN, the results show that phenolic hydroxyl groups and two benzene rings interact with HIV-IN and are possible pharmacodynamic groups.
- Published
- 2024
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