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Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

Publication ,  Journal Article
Tian, X; Qin, B; Wu, Z; Wang, X; Lu, H; Morris-Natschke, SL; Chen, CH; Jiang, S; Lee, K-H; Xie, L
Published in: J Med Chem
December 9, 2010

On the basis of the structures and activities of our previously identified non-nucleoside reverse transcriptase inhibitors (NNRTIs), we designed and synthesized two sets of derivatives, diarylpyridines (A) and diarylanilines (B), and tested their anti-HIV-1 activity against infection by HIV-1 NL4-3 and IIIB in TZM-bl and MT-2 cells, respectively. The results showed that most compounds exhibited potent anti-HIV-1 activity with low nanomolar EC50 values, and some of them, such as 13m, 14c, and 14e, displayed high potency with subnanomolar EC50 values, which were more potent than etravirine (TMC125, 1) in the same assays. Notably, these compounds were also highly effective against infection by multi-RTI-resistant strains, suggesting a high potential to further develop these compounds as a novel class of NNRTIs with improved antiviral efficacy and resistance profile.

Duke Scholars

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Published In

J Med Chem

DOI

EISSN

1520-4804

Publication Date

December 9, 2010

Volume

53

Issue

23

Start / End Page

8287 / 8297

Location

United States

Related Subject Headings

  • Reverse Transcriptase Inhibitors
  • Pyridines
  • Models, Molecular
  • Microbial Sensitivity Tests
  • Medicinal & Biomolecular Chemistry
  • Mass Spectrometry
  • Magnetic Resonance Spectroscopy
  • Humans
  • HIV-1
  • HIV Reverse Transcriptase
 

Citation

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Tian, X., Qin, B., Wu, Z., Wang, X., Lu, H., Morris-Natschke, S. L., … Xie, L. (2010). Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. J Med Chem, 53(23), 8287–8297. https://doi.org/10.1021/jm100738d
Tian, Xingtao, Bingjie Qin, Zhiyuan Wu, Xiaofeng Wang, Hong Lu, Susan L. Morris-Natschke, Chin Ho Chen, Shibo Jiang, Kuo-Hsiung Lee, and Lan Xie. “Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.J Med Chem 53, no. 23 (December 9, 2010): 8287–97. https://doi.org/10.1021/jm100738d.
Tian X, Qin B, Wu Z, Wang X, Lu H, Morris-Natschke SL, et al. Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. J Med Chem. 2010 Dec 9;53(23):8287–97.
Tian, Xingtao, et al. “Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.J Med Chem, vol. 53, no. 23, Dec. 2010, pp. 8287–97. Pubmed, doi:10.1021/jm100738d.
Tian X, Qin B, Wu Z, Wang X, Lu H, Morris-Natschke SL, Chen CH, Jiang S, Lee K-H, Xie L. Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. J Med Chem. 2010 Dec 9;53(23):8287–8297.
Journal cover image

Published In

J Med Chem

DOI

EISSN

1520-4804

Publication Date

December 9, 2010

Volume

53

Issue

23

Start / End Page

8287 / 8297

Location

United States

Related Subject Headings

  • Reverse Transcriptase Inhibitors
  • Pyridines
  • Models, Molecular
  • Microbial Sensitivity Tests
  • Medicinal & Biomolecular Chemistry
  • Mass Spectrometry
  • Magnetic Resonance Spectroscopy
  • Humans
  • HIV-1
  • HIV Reverse Transcriptase