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BioAssay: AID 1062975

Inhibition of human recombinant glutathione reductase using glutathione as substrate preincubated for 30 mins by colorimetric assay

A series of bis-(arylmethylidene)-cycloalkanones was synthesized by cross-aldol condensation. The activity of the compounds was evaluated against amastigotes forms of Trypanosoma cruzi and promastigotes forms of Leishmania amazonensis. The cytotoxicity of the active compounds on uninfected fibroblasts or macrophages was established in vitro to evaluate the selectivity of their antiparasitic more ..
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 Tested Compounds
 Tested Compounds
All(8)
 
 
Active(1)
 
 
Unspecified(7)
 
 
 Tested Substances
 Tested Substances
All(8)
 
 
Active(1)
 
 
Unspecified(7)
 
 
AID: 1062975
Data Source: ChEMBL (1284129)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
Deposit Date: 2014-08-22

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Glutathione reductase, mitochondrial; Short=GR; Short=GRase; Flags: Precursor
Description ..   
Protein Family: Pyridine nucleotide-disulphide oxidoreductase, dimerization domain
Comment ..   

Gene:GSR     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
Description:
Title: Synthesis and evaluation of the antiparasitic activity of bis-(arylmethylidene) cycloalkanones.

Abstract: A series of bis-(arylmethylidene)-cycloalkanones was synthesized by cross-aldol condensation. The activity of the compounds was evaluated against amastigotes forms of Trypanosoma cruzi and promastigotes forms of Leishmania amazonensis. The cytotoxicity of the active compounds on uninfected fibroblasts or macrophages was established in vitro to evaluate the selectivity of their antiparasitic effects. Six compounds displayed trypanocidal activity against amastigotes intracellular forms of T. cruzi with IC## values ranging from 7.0 to 249 muM. Besides these six compounds, eight other molecules exhibited significant leishmanicidal activity (IC## values ranging from 0.6 to 110.4 muM). Two compounds can be considered as promising antiparasitic lead molecules because they showed IC## values in the low-micromolar range (#1.2 muM) with an adequate SI (#19.9). To understand the mechanism of action of these compounds, two possible molecular targets were investigated: trypanothione reductase (TR) and cruzain.
(PMID: 24321832)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Protein Target Class: enzyme reductase
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2IC50 activity commentIC50 activity commentString
3IC50 standard flagIC50 standard flagInteger
4IC50 qualifierIC50 qualifierString
5IC50 published valueIC50 published valueFloatμM
6IC50 standard valueIC50 standard valueFloatnM
7IC50 data validityIC50 data validityString

* Activity Concentration.

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
Classification
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