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New phorbol ester derivatives as potent anti-HIV agents.

Publication ,  Journal Article
Li, Q-R; Cheng, Y-Y; Zhao, L; Huang, X-L; Jiang, X-G; Cui, Y-D; Morris-Natschke, SL; Goto, M; Chen, C-H; Lee, K-H; Chen, D-F; Zhang, J
Published in: Bioorg Med Chem Lett
October 15, 2021

Tigliane esters show many biological activities, including anti-HIV-1 activity. Our aim in this study was to establish structure-anti-HIV activity relationships for four series of tigliane-type diterpenoids. We synthesized and evaluated 29 new phorbol ester derivatives for anti-HIV activity and for cytotoxicity against human tumor cell lines. Among them, three derivatives, two phorbol-13-monoesters (5d and 5e) and a phorbol-12,13-diester (6a), showed significant anti-HIV activity. We found that better anti-HIV activity was often associated with a shorter acyl ester at C-13. Particularly, compounds with a phenyl ring in the ester side chain exhibited excellent anti-HIV activity and had good safety indexes. Due to its significant anti-HIV potency with a high selectivity index, phorbol-12,13-dicinnamoate (6a) was chosen as the potential candidate for further preclinical trials.

Duke Scholars

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Published In

Bioorg Med Chem Lett

DOI

EISSN

1464-3405

Publication Date

October 15, 2021

Volume

50

Start / End Page

128319

Location

England

Related Subject Headings

  • Virus Replication
  • Structure-Activity Relationship
  • Phorbol Esters
  • Molecular Structure
  • Medicinal & Biomolecular Chemistry
  • Humans
  • HIV-1
  • Cell Survival
  • Cell Line, Tumor
  • Antineoplastic Agents
 

Citation

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MLA
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Li, Q.-R., Cheng, Y.-Y., Zhao, L., Huang, X.-L., Jiang, X.-G., Cui, Y.-D., … Zhang, J. (2021). New phorbol ester derivatives as potent anti-HIV agents. Bioorg Med Chem Lett, 50, 128319. https://doi.org/10.1016/j.bmcl.2021.128319
Li, Qi-Run, Yung-Yi Cheng, Lei Zhao, Xiao-Lei Huang, Xiao-Gang Jiang, Ya-Dong Cui, Susan L. Morris-Natschke, et al. “New phorbol ester derivatives as potent anti-HIV agents.Bioorg Med Chem Lett 50 (October 15, 2021): 128319. https://doi.org/10.1016/j.bmcl.2021.128319.
Li Q-R, Cheng Y-Y, Zhao L, Huang X-L, Jiang X-G, Cui Y-D, et al. New phorbol ester derivatives as potent anti-HIV agents. Bioorg Med Chem Lett. 2021 Oct 15;50:128319.
Li, Qi-Run, et al. “New phorbol ester derivatives as potent anti-HIV agents.Bioorg Med Chem Lett, vol. 50, Oct. 2021, p. 128319. Pubmed, doi:10.1016/j.bmcl.2021.128319.
Li Q-R, Cheng Y-Y, Zhao L, Huang X-L, Jiang X-G, Cui Y-D, Morris-Natschke SL, Goto M, Chen C-H, Lee K-H, Chen D-F, Zhang J. New phorbol ester derivatives as potent anti-HIV agents. Bioorg Med Chem Lett. 2021 Oct 15;50:128319.
Journal cover image

Published In

Bioorg Med Chem Lett

DOI

EISSN

1464-3405

Publication Date

October 15, 2021

Volume

50

Start / End Page

128319

Location

England

Related Subject Headings

  • Virus Replication
  • Structure-Activity Relationship
  • Phorbol Esters
  • Molecular Structure
  • Medicinal & Biomolecular Chemistry
  • Humans
  • HIV-1
  • Cell Survival
  • Cell Line, Tumor
  • Antineoplastic Agents