Abstract:
:Formazan-based colorimetric cytotoxicity assays, such as the MTT assay, are typically used to assess cell viability with only metabolically active cells reducing tetrazolium salts into the formazans, which is then quantified by absorbance. Fluorescence offers several advantages compared to colorimetric assays and would enable techniques such as flow cytometry and confocal microscopy to be used for analysis. Here, fluorescent formazans 10, 11 and 12, and their corresponding tetrazolium salts 13, 16 and 24, respectively, were synthesised by incorporation of a known fluorophore backbone (coumarin, fluorescein and rhodol) with disruption of the conjugated system preventing or reducing fluorescence of the tetrazolium salts. These tetrazolium salts were successfully reduced to the fluorescent formazans with cells and offer a step forward in the development of fluorescent cytotoxicity assays.
journal_name
Comb Chem High Throughput Screenjournal_title
Combinatorial chemistry & high throughput screeningauthors
Ladyman MK,Walton JG,Lilienkampf A,Bradley Mdoi
10.2174/1386207319666160408150913subject
Has Abstractpub_date
2016-01-01 00:00:00pages
384-91issue
5eissn
1386-2073issn
1875-5402pii
CCHTS-EPUB-74869journal_volume
19pub_type
杂志文章abstract:BACKGROUND:Diabetes mellitus is one of the most common endocrine metabolic disorder diseases. The application of herbal medicine to control glucose levels and improve insulin action might be a useful approach in the treatment of diabetes. Mulberry leaves (ML) has been reported to exert important activities of anti-diab...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:10.2174/1386207323666200914103719
更新日期:2020-09-13 00:00:00
abstract::Therapeutic options for many infections are extremely limited and at crisis point. We run the risk of entering a second pre-antibiotic era. There had been no miracle drug for the patients infected by resistant microbial pathogens. Most of the very few new drugs under development have problems with their toxicity, or p...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章,评审
doi:10.2174/13862073113166660065
更新日期:2014-01-01 00:00:00
abstract::African trypanosomes are extracellular blood parasites that cause sleeping sickness in humans and Nagana in cattle. The therapeutics used to control and treat these diseases are very ineffective and thus, the development of new drugs is urgently needed. We have previously suggested to use trypanosome-specific RNA apta...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:10.2174/138620706777935324
更新日期:2006-08-01 00:00:00
abstract::Bacteriophage (phage) display has been exploited for the purpose of discovering new cancer specific targeting peptides. However, this approach has resulted in only a small number of tumor targeting peptides useful as in vivo imaging agents. We hypothesize that in vivo screening for tumor uptake of fluorescently tagged...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:10.2174/1386207311107010009
更新日期:2011-01-01 00:00:00
abstract::A new and simple high-performance liquid chromatography method was developed and validated for the simultaneous determination of retinol, retinyl palmitate, β-carotene, α-tocopherol and vitamin C in rat serum treated with Plantago Major L. and 7,12 dimethylbenz[a]anthracene. High-performance liquid chromatography anal...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:
更新日期:2013-02-01 00:00:00
abstract::Building accurate quantitative structure-activity relationships (QSAR) is important in drug design, environmental modeling, toxicology, and chemical property prediction. QSAR methods can be utilized to solve mainly two types of problems viz., pattern recognition, (or classification) where output is discrete (i.e. clas...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章,评审
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abstract::NMR has proven to be a valuable tool for identifying small molecule drug leads that serve as starting points for lead optimization programs. In addition, NMR screening can also be applied during lead optimization in order to improve the pharmacokinetic properties of a compound. In this paper we review the NMR methods ...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章,评审
doi:10.2174/1386207023329941
更新日期:2002-12-01 00:00:00
abstract:AIM AND OBJECTIVE:Actinomycetes produce structurally unique secondary metabolites with pharmaceutically essential bioactivities. Salinispora, an obligate marine actinomycete, produces structurally varied and unique secondary metabolites. There is plenty of scope for development of drugs from the novel compounds isolate...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:10.2174/1386207319666161215154128
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abstract::A pulsed ultrafiltration-mass spectrometric screening assay has been developed to generate and identify electrophilic metabolites of xenobiotic compounds formed by hepatic cytochrome P450 enzymes. This assay would be suitable for the early identification of potentially toxic compounds during the initial phase of drug ...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:
更新日期:1999-06-01 00:00:00
abstract::4-Benzothiazol-2-ylamino-4-oxo-2-butenoic acid, prepared from reaction of 2-aminobenzothiazole and maleic anhydride, are used as an acid component in Passerini three-component reaction, under solvent-free media, to produce unsaturated α-benzothiazole acyloxyamides in good yields. ...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:10.2174/13862073113169990041
更新日期:2013-11-01 00:00:00
abstract::Clinical application of viral vectors is often hampered by the lack of selectivity of viral particles for the targeted tissue. This drawback decreases the efficiency of gene delivery and raises safety concerns. We successfully established a novel in vitro evolution protocol to engineer adeno-associated virus vectors w...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:10.2174/138620710792927385
更新日期:2010-11-01 00:00:00
abstract::Lipopolysaccharides (LPS), otherwise termed 'endotoxins', are outer-membrane constituents of Gram-negative bacteria. Lipopolysaccharides play a key role in the pathogenesis of 'Septic Shock', a major cause of mortality in the critically ill patient. Therapeutic options aimed at limiting downstream systemic inflammator...
journal_title:Combinatorial chemistry & high throughput screening
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更新日期:2004-05-01 00:00:00
abstract::African trypanosomes are the causative agent of sleeping sickness. The therapeutics used to control and treat the disease are very ineffective and thus, the development of improved drugs is urgently needed. Recently, new strategies for the design of novel trypanocidals have been put forward. Among them are techniques ...
journal_title:Combinatorial chemistry & high throughput screening
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更新日期:2008-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVE:Swertia mussotii Franch, also known as "Zangyinchen", is one of a Tibetan traditional herb used for treatment of liver diseases over thousands of years at Qinghai-Tibet Plateau, has been confirmed to be hepatoprotective. However, the underlying mechanism is largely unknown. MATERIALS AND METHO...
journal_title:Combinatorial chemistry & high throughput screening
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doi:10.2174/1386207322666191106105725
更新日期:2019-01-01 00:00:00
abstract:AIM AND OBJECTIVE:The present method is simple, green and highly efficient for the synthesis of 2-amino-4H-pyran derivatives which are achieved by a one pot three component cyclocondensation of aldehyde, malanonitrile and ethyl acetoacetate or methyl acetoacetate using DABCO under solvent free with grinding conditions ...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:10.2174/1386207321666180315095422
更新日期:2018-01-01 00:00:00
abstract::In the life cycle of hepatitis C virus (HCV), NS3/NS4A protease has been proved to play a vital role in the replication of the HCV virus. Narlaprevir and its derivatives, the inhibitors of NS3/NS4A, would be potentially developed as important anti-HCV drugs in the future. In this study, quantitative structure-activity...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:10.2174/138620712800563918
更新日期:2012-07-01 00:00:00
abstract::Quantitative structure-activity relationships (QSARs) have important applications in drug discovery research, environmental fate modeling, property prediction, etc. Validation has been recognized as a very important step for QSAR model development. As one of the important objectives of QSAR modeling is to predict acti...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章,评审
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更新日期:2011-07-01 00:00:00
abstract::Fingerprint representations of molecular structure and properties were among the first computational tools for similarity searching and are widely applied to this date, which is in part due to their computational efficiency and ease-of-use. Moreover, despite their simplicity, 2D molecular fingerprints have been surpri...
journal_title:Combinatorial chemistry & high throughput screening
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更新日期:2010-03-01 00:00:00
abstract::Protein Kinase C βII (PKCβII) overexpression has been linked to various diabetic microvascular complications viz. retinopathy, neuropathy, and cardiomyopathy. Novel and potent small molecules with preferential selective inhibitory property of PKCβII will be helpful in treatment as well as understanding insight of PKCβ...
journal_title:Combinatorial chemistry & high throughput screening
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更新日期:2014-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVE:Perimenopause is a physiological occurrence in women, and is characterized by endocrine and biochemical changes. During perimenopause phase, many derangements or abnormal health conditions start developing as a result of hormonal changes. These derangements in health conditions and biochemical ...
journal_title:Combinatorial chemistry & high throughput screening
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更新日期:2020-10-23 00:00:00
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journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章,评审
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更新日期:2011-03-01 00:00:00
abstract::Multicomponent reactions (MCRs) generate multiple bonds in a single reaction process, which is highly efficient to construct relatively complex molecules. Conducting post-MCR modification reactions further increases the molecular complexity and diversity. MCR has become a powerful approach to make drug-like molecules ...
journal_title:Combinatorial chemistry & high throughput screening
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更新日期:2007-03-01 00:00:00
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journal_title:Combinatorial chemistry & high throughput screening
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更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:Clinical outcomes after rotator cuff repair associated with diabetes mellitus(DM) are generally favorable, but no study has attempted to establish the influence of DM on outcomes after rotator cuff repair. PURPOSE:To conduct a meta-analysis of clinical studies evaluating patient outcomes between people with...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: meta分析
doi:10.2174/1386207323666201020114034
更新日期:2020-10-20 00:00:00
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journal_title:Combinatorial chemistry & high throughput screening
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更新日期:2014-01-01 00:00:00
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journal_title:Combinatorial chemistry & high throughput screening
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更新日期:2010-09-01 00:00:00
abstract:Aims & Objective:Corona Virus Disease 2019 (COVID-19) caused by the human coronavirus 2019 (HCoV-19, also known as SARS-CoV-2) infection is currently in a global outbreak. COVID-19 has posed a huge threat to public health and economic stability worldwide. CR3022, a human monoclonal neutralizing antibody isolated from a...
journal_title:Combinatorial chemistry & high throughput screening
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更新日期:2020-10-26 00:00:00
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journal_title:Combinatorial chemistry & high throughput screening
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更新日期:2004-02-01 00:00:00
abstract::Growth hormone secretagogues (GHSs) are synthetic molecules that stimulate and amplify pulsatile pituitary growth hormone release, via a separate pathway distinct from GH releasing hormone/somatostatin. The activity of GHSs is not fully specific for GH secretion; some GHSs also have slight releasing activity on other ...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章,评审
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更新日期:2006-03-01 00:00:00
abstract:AIMS AND OBJECTIVE:Alzheimer's disease is now a most prevalent neuro degenerative disease of central nervous system leading to dementia in elderly aged population. Numerous pathological changes have been associated in the progression of Alzheimer's disease. One of such pathological hypothesis is declined cholinergic ac...
journal_title:Combinatorial chemistry & high throughput screening
pub_type: 杂志文章
doi:10.2174/1386207323666201211092138
更新日期:2020-12-10 00:00:00