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Chemical Structure| 617-86-7 Chemical Structure| 617-86-7

Structure of Triethylsilane
CAS No.: 617-86-7

Chemical Structure| 617-86-7

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Product Citations

Product Citations

Wisam A. Dawood ; Gillian M. Fisher ; Franziska J.M. Kinnen ; Christian Anzenhofer ; Tina Skinner-Adams ; Leandro Alves Avelar , et al.

Abstract: There are more than 240 million cases of malaria and 600,000 associated deaths each year, most due to infection with Plasmodium falciparum parasites. While malaria treatment options exist, new drugs with novel modes of action are needed to address malaria parasite drug resistance. Protein lysine deacetylases (termed HDACs) are important epigenetic regulatory enzymes and prospective therapeutic targets for malaria. Here we report the antiplasmodial activity of a panel of 17 hydroxamate zinc binding group HDAC inhibitors with alkoxyamide linkers and different cap groups. The two most potent compounds (4a and 4b) were found to inhibit asexual P. falciparum growth with 50% inhibition concentrations (IC50's) of 0.07 μM and 0.09 μM, respectively, and demonstrated >200-fold more selectivity for P. falciparum parasites versus human neonatal foreskin fibroblasts (NFF). In situ hyperacetylation studies demonstrated that 4a, 4b and analogs caused P. falciparum histone H4 hyperacetylation, suggesting HDAC inhibition, with structure activity relationships providing information relevant to the design of new Plasmodium-specific aliphatic chain hydroxamate HDAC inhibitors.

Keywords: HDAC inhibitor ; Malaria ; P. falciparum ; Antiplasmodial

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Product Details of [ 617-86-7 ]

CAS No. :617-86-7
Formula : C6H16Si
M.W : 116.28
SMILES Code : CC[SiH](CC)CC
MDL No. :MFCD00009018
InChI Key :QXTIBZLKQPJVII-UHFFFAOYSA-N
Pubchem ID :6327258

Safety of [ 617-86-7 ]

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H225-H315-H319
Precautionary Statements:P210-P233-P240-P241+P242+P243-P264-P280-P302+P352+P332+P313+P362+P364-P305+P351+P338+P337+P313-P370+P378-P403+P235-P501
Class:3
UN#:1993
Packing Group:

Application In Synthesis of [ 617-86-7 ]

* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.

  • Upstream synthesis route of [ 617-86-7 ]
  • Downstream synthetic route of [ 617-86-7 ]

[ 617-86-7 ] Synthesis Path-Upstream   1~1

  • 1
  • [ 617-86-7 ]
  • [ 5580-79-0 ]
  • [ 358-43-0 ]
  • [ 66684-57-9 ]
References: [1] Journal of the American Chemical Society, 2012, vol. 134, # 39, p. 16216 - 16227,12.
 

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