Synthesis and anti-HIV activities of phorbol derivatives.

12-(Trans-4-fluorocinnamoyl)-13-decanoyl phorbol Anti-HIV-1 activity HIV-1 entry inhibitor HIV-1 reverse transcriptase inhibitor PKC activator Phorbol esters Safety index Syncytia formation

Journal

Chinese journal of natural medicines
ISSN: 1875-5364
Titre abrégé: Chin J Nat Med
Pays: China
ID NLM: 101504416

Informations de publication

Date de publication:
Feb 2024
Historique:
received: 19 08 2023
medline: 12 2 2024
pubmed: 12 2 2024
entrez: 11 2 2024
Statut: ppublish

Résumé

In this study, 37 derivatives of phorbol esters were synthesized and their anti-HIV-1 activities evaluated, building upon our previous synthesis of 51 phorbol derivatives. 12-Para-electron-acceptor-trans-cinnamoyl-13-decanoyl phorbol derivatives stood out, demonstrating remarkable anti-HIV-1 activities and inhibitory effects on syncytia formation. These derivatives exhibited a higher safety index compared with the positive control drug. Among them, 12-(trans-4-fluorocinnamoyl)-13-decanoyl phorbol, designated as compound 3c, exhibited the most potent anti-HIV-1 activity (EC

Identifiants

DOI: 10.1016/S1875-5364(24)60587-X PMID: 38342567
pubmed: 38342567
pii: S1875-5364(24)60587-X
doi: 10.1016/S1875-5364(24)60587-X
pii:
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

146-160

Informations de copyright

Copyright © 2024 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.

Auteurs

Xiaolei Huang (X)

College of Pharmaceutical Science, Soochow University, Suzhou 215123, China.

Chengrun Tang (C)

Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences/Key Laboratory of Bioactive Peptides of Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China.

Xusheng Huang (X)

Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences/Key Laboratory of Bioactive Peptides of Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China; Kunming College of Life Science, University of Chinese Academy of Sciences, Kunming, Yunnan 650204, China.

Yun Yang (Y)

College of Pharmaceutical Science, Soochow University, Suzhou 215123, China.

Qirun Li (Q)

College of Pharmaceutical Science, Soochow University, Suzhou 215123, China.

Mengdi Ma (M)

Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences/Key Laboratory of Bioactive Peptides of Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China.

Lei Zhao (L)

College of Pharmaceutical Science, Soochow University, Suzhou 215123, China.

Liumeng Yang (L)

Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences/Key Laboratory of Bioactive Peptides of Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China.

Yadong Cui (Y)

College of Pharmaceutical Science, Soochow University, Suzhou 215123, China.

Zhenqing Zhang (Z)

College of Pharmaceutical Science, Soochow University, Suzhou 215123, China. Electronic address: z_zhang@suda.edu.cn.

Yongtang Zheng (Y)

Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences/Key Laboratory of Bioactive Peptides of Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China; Kunming College of Life Science, University of Chinese Academy of Sciences, Kunming, Yunnan 650204, China. Electronic address: zhengyt@mail.kiz.ac.cn.

Jian Zhang (J)

College of Pharmaceutical Science, Soochow University, Suzhou 215123, China. Electronic address: jianzhang@suda.edu.cn.

Classifications MeSH