Advanced search
1 file | 138.49 KB Add to list

Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents

(2017) FUTURE MEDICINAL CHEMISTRY. 9(4). p.357-364
Author
Organization
Abstract
Aim: The recurring resistance of the malaria parasite to many drugs compels the design of innovative chemical entities in antimalarial research. Pan- histone deacetylase inhibitors (pan-HDACis) have recently been presented in the literature as powerful novel antimalarials, although their application is hampered due to toxic side effects. This drawback might be neutralized by the deployment of isoformselective HDACis. Results: In this study, 42 thiaheterocyclic benzohydroxamic acids, 17 of them being potent and selective hHDAC6 inhibitors, were tested to investigate a possible correlation between hHDAC6 inhibition and antiplasmodial activity. Conclusion: Four hHDAC6 inhibitors showed submicromolar potency against both a chloroquine- sensitive and a chloroquine-resistant strain of Plasmodium falciparum with high selectivity indices, pointing to the relevance of exploring hHDAC6 inhibitors as potential new antiplasmodial agents.
Keywords
benzohydroxamic acids, HDAC6, malaria, Plasmodium falciparum, thiaheterocycles, SELECTIVE HDAC6 INHIBITORS, PLASMODIUM-FALCIPARUM, HISTONE DEACETYLASES, ASSAY, IDENTIFICATION, DISCOVERY, PARASITES, THERAPY, DISEASE, ANALOGS

Downloads

  • Antimalarial hHDAC6i - REVISED ms.docx
    • full text
    • |
    • open access
    • |
    • Word
    • |
    • 138.49 KB

Citation

Please use this url to cite or link to this publication:

MLA
De Vreese, Rob et al. “Exploration of Thiaheterocyclic hHDAC6 Inhibitors as Potential Antiplasmodial Agents.” FUTURE MEDICINAL CHEMISTRY 9.4 (2017): 357–364. Print.
APA
De Vreese, R., de Kock, C., Smith, P. J., Chibale, K., & D’hooghe, M. (2017). Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents. FUTURE MEDICINAL CHEMISTRY, 9(4), 357–364.
Chicago author-date
De Vreese, Rob, Carmen de Kock, Peter J Smith, Kelly Chibale, and Matthias D’hooghe. 2017. “Exploration of Thiaheterocyclic hHDAC6 Inhibitors as Potential Antiplasmodial Agents.” Future Medicinal Chemistry 9 (4): 357–364.
Chicago author-date (all authors)
De Vreese, Rob, Carmen de Kock, Peter J Smith, Kelly Chibale, and Matthias D’hooghe. 2017. “Exploration of Thiaheterocyclic hHDAC6 Inhibitors as Potential Antiplasmodial Agents.” Future Medicinal Chemistry 9 (4): 357–364.
Vancouver
1.
De Vreese R, de Kock C, Smith PJ, Chibale K, D’hooghe M. Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents. FUTURE MEDICINAL CHEMISTRY. 2017;9(4):357–64.
IEEE
[1]
R. De Vreese, C. de Kock, P. J. Smith, K. Chibale, and M. D’hooghe, “Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents,” FUTURE MEDICINAL CHEMISTRY, vol. 9, no. 4, pp. 357–364, 2017.
@article{8541550,
  abstract     = {Aim: The recurring resistance of the malaria parasite to many drugs compels the design of innovative chemical entities in antimalarial research. Pan- histone deacetylase inhibitors (pan-HDACis) have recently been presented in the literature as powerful novel antimalarials, although their application is hampered due to toxic side effects. This drawback might be neutralized by the deployment of isoformselective HDACis.
Results: In this study, 42 thiaheterocyclic benzohydroxamic acids, 17 of them being potent and selective hHDAC6 inhibitors, were tested to investigate a possible correlation between hHDAC6 inhibition and antiplasmodial activity.
Conclusion: Four hHDAC6 inhibitors showed submicromolar potency against both a chloroquine- sensitive and a chloroquine-resistant strain of Plasmodium falciparum with high selectivity indices, pointing to the relevance of exploring hHDAC6 inhibitors as potential new antiplasmodial agents.},
  author       = {De Vreese, Rob and de Kock, Carmen and Smith, Peter J and Chibale, Kelly and D'hooghe, Matthias},
  issn         = {1756-8919},
  journal      = {FUTURE MEDICINAL CHEMISTRY},
  keywords     = {benzohydroxamic acids,HDAC6,malaria,Plasmodium falciparum,thiaheterocycles,SELECTIVE HDAC6 INHIBITORS,PLASMODIUM-FALCIPARUM,HISTONE DEACETYLASES,ASSAY,IDENTIFICATION,DISCOVERY,PARASITES,THERAPY,DISEASE,ANALOGS},
  language     = {eng},
  number       = {4},
  pages        = {357--364},
  title        = {Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents},
  url          = {http://dx.doi.org/10.4155/fmc-2016-0215},
  volume       = {9},
  year         = {2017},
}

Altmetric
View in Altmetric
Web of Science
Times cited: