A Convenient Method for the Synthesis of Chromeno[4,3-b]pyridines Via Three-component Reaction.

abstract：:Recent studies have suggested that both constitutive androstane receptor (CAR) and pregnane X-receptor (PXR) are involved in the induction of rat liver microsomal cytochrome P-450 (CYP) 2B and 3A through a mechanism called cross-talk. In this study we intend to determine if a PXR-reporter gene assay could be used for ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Cui X,Thomas A,Montgomery D,Gu C,Morrison RA,White RE,Cheng KC

更新日期：2005-06-01 00:00:00

abstract：:We have developed a high throughput assay for the measurement of protease activity in solution. This technology will accelerate research in functional proteomics and enable biologists to streamline protease substrate evaluation and optimization. The peptide sequences that serve as protease substrates in this assay are...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kozlov IA,Melnyk PC,Zhao C,Hachmann JP,Shevchenko V,Srinivasan A,Barker DL,Lebl M

更新日期：2006-07-01 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

authors： Macha B,Kulkarni R,Garige AK,Palabindala R,Akkinepally R,Garlapati A

更新日期：2020-12-10 00:00:00

abstract：AIMS AND OBJECTIVE:The infectious disease treatment remains a challenging concern owing to the increasing number of pathogenic microorganisms associated with resistance to multiple drugs. A promising approach for combating microbial infection is to combine two or more known bioactive heterocyclic pharmacophores in one ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Tratrat C

更新日期：2020-01-01 00:00:00

abstract：:Cell-based screening using phenotypic assays is a useful means of identifying bioactive chemicals for use as tools to elucidate complex cellular processes. However, the chemicals must display sufficient selectivity and their targets have to be identified. We describe how cell-based screening assays can be designed to ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Schriemer DC,Kemmer D,Roberge M

更新日期：2008-09-01 00:00:00

abstract：BACKGROUND:Neurofibromatosis, also known as Von Recklinghausen disease, is a systemic and progressive genetic disease that primarily affects the skin, eyes, nervous system and bones. The disease can occur in a variety of ways and can vary from individuals. Metabolomic-based research using blood samples has enabled new ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Oz O,Koyuncu I,Gonel A

更新日期：2020-12-04 00:00:00

abstract：:Organic reactions performed in the absence of solvent in domestic ovens without appropriate temperature control are generally considered as not reproducible, particularly when different instruments are used. For this reason, reproducibility has historically been one of the major issues associated with Microwave-Assist...

journal_title：Combinatorial chemistry & high throughput screening

authors： Díaz-Ortiz A,de la Hoz A,Alcázar J,Carrillo JR,Herrero MA,Fontana A,Muñoz Jde M,Prieto P,de Cózar A

更新日期：2011-02-01 00:00:00

abstract：:Increasingly, combinatorial libraries are used to screen large numbers of complex chemically- and physically-patterned polymers against cell response. There is a strong need to extract meaningful relationships between cell function and material surface features from these experiments. A novel high-throughput cell-mate...

journal_title：Combinatorial chemistry & high throughput screening

authors： Su J,Meredith JC

更新日期：2009-07-01 00:00:00

abstract：:Virtual screening encompasses a wide range of computational approaches aimed at the high-throughput, cost-efficient exploration of chemical libraries or databases to discover new bioactive compounds or novel medical indications of known drugs. Here, we have performed a systematic comparison of the performance of a lar...

journal_title：Combinatorial chemistry & high throughput screening

authors： Di Ianni ME,Gantner ME,Ruiz ME,Castro EA,Bruno-Blanch LE,Talevi A

更新日期：2015-01-01 00:00:00

abstract：:Historically, most bioanalytical methods for drug analysis in pharmaceutical industry were developed using HPLC coupled with UV or fluorescence detection. However, there is a trend toward interfacing separation technologies with more sensitive tandem mass spectrometry (MS/MS)-based systems. MS/MS detection offers comp...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hsieh Y,Fukuda E,Wingate J,Korfmacher WA

更新日期：2006-01-01 00:00:00

abstract：:Trivalent lanthanide ions (Ln(3+)) doped inorganic nanocrystals (NCs) have currently attracted reviving interest and come to the forefront in nanophotonics owing to their potential applications in diverse fields such as luminescent biodetection and bioimaging. As an alternative to conventional biolabels, Ln(3+)-doped ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ju Q,Tu D,Liu Y,Zhu H,Chen X

更新日期：2012-08-01 00:00:00

abstract：:Recently, we established a robust method for the detection of hybridization events using a DNA microarray deposited on a nanoporous membrane. Here, in a follow-up study, we demonstrate the performance of this approach on a larger set of LNA-modified oligoprobes and genomic DNA sequences. Twenty-six different LNA-modif...

journal_title：Combinatorial chemistry & high throughput screening

authors： Liu JP,Drungowski M,Nyársik L,Schwartz R,Lehrach H,Herwig R,Janitz M

更新日期：2007-05-01 00:00:00

abstract：:Mass spectrometric plasma analysis for biomarker discovery has become an exploratory focus in proteomic research: the challenges of analyzing plasma samples by mass spectrometry have become apparent not only since the human proteome organization (HUPO) has put much emphasis on the human plasma proteome. This work demo...

journal_title：Combinatorial chemistry & high throughput screening

authors： Tammen H,Hess R,Schulte I,Kellmann M,Appel A,Budde P,Zucht HD,Schulz-Knappe P

更新日期：2005-12-01 00:00:00

abstract：OBJECTIVE:A significant proportion of patients with early non-small cell lung cancer (NSCLC) can be cured by surgery. The distant metastasis of tumors is the most common cause of treatment failure. Precisely predicting the likelihood that a patient develops distant metastatic risk will help identify patients who can fu...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zhong J,Chen JM,Chen SL,Yi YF

更新日期：2019-01-01 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

authors： Lu X,Sun H,Xu Y,Cao X

更新日期：2020-10-20 00:00:00

abstract：:Among the various parasitic diseases, malaria is the deadliest one. Due to the emergence of high drug resistance to the existing drug candidates there is a global need for development of new drug candidates which will be effective against resistant strains of malaria parasite. In silico molecular modeling approaches h...

journal_title：Combinatorial chemistry & high throughput screening

authors： Barmade MA,Murumkar PR,Sharma MK,Shingala KP,Giridhar RR,Yadav MR

更新日期：2015-01-01 00:00:00

abstract：:In recent years, a trend of change has been observed within pharmaceutical industry. As modern drug discovery has reached a remarkable level of complexity and drugs need to be discovered, developed and produced against strict timelines and within cost- and regulatory constraints, industry seeks "lean" solutions to inc...

journal_title：Combinatorial chemistry & high throughput screening

authors： Pieters S,Dejaegher B,Vander Heyden Y

更新日期：2010-07-01 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

authors： Grewal BK,Sobhia ME

更新日期：2014-01-01 00:00:00

abstract：AIM AND OBJECTIVE:Avicularin has been found to inhibit the proliferation of HepG-2 cells in vitro in the screening of our laboratory. We intended to explain the molecular mechanism of this effect. Therefore, the combined methods of reverse molecular docking and network pharmacology were used in order to illuminate the ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Duan C,Li Y,Dong X,Xu W,Ma Y

更新日期：2019-01-01 00:00:00

abstract：AIM AND OBJECTIVE:The rapid increase in the amount of protein sequence data available leads to an urgent need for novel computational algorithms to analyze and compare these sequences. This study is undertaken to develop an efficient computational approach for timely encoding protein sequences and extracting the hidden...

journal_title：Combinatorial chemistry & high throughput screening

authors： Li C,Zhao J,Wang C,Yao Y

更新日期：2018-01-01 00:00:00

abstract：:Sequential injection analysis (SIA) has been employed as the platform for the development of a high throughput automated assay for glutathione (GSH) in nutrition supplements. The proposed assay is based on the on-line formation of a UV-absorbing thioacrylate derivative (lambda(max) = 285 nm) upon reaction of thiol wit...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zacharis CK,Tzanavaras PD

更新日期：2010-07-01 00:00:00

abstract：:Development of calcium channel blockers is attractive, but has in the past been hampered by lack of high throughput electrophysiological technology. This limitation has been overcome by the implementation of automated patch clamp systems that allow identification of state-dependent compounds, which preferentially targ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hermann D,Mezler M,Swensen AM,Bruehl C,Obergrußerger A,Wicke K,Schoemaker H,Gross G,Draguhn A,Nimmrich V

更新日期：2013-03-01 00:00:00

abstract：:Two tryptophan-modified permethylated beta-cyclodextrins, 6I-L-Trp-6I-deoxy-2I,3I-di-O-methyl-hexakis(2II-VII,3II-VII,6II-VII-tri-O-methyl-beta-cyclodextrin (3) and 6I-D-Trp- 6I-deoxy-2I,3I-di-O-methyl-hexakis(2II-VII,3II-VII,6II-VII-tri-O-methyl)-beta-cyclodextrin (4), were synthesized, and their binding behaviors we...

journal_title：Combinatorial chemistry & high throughput screening

authors： Liu Y,Kang S,Chen Y,Shi J,Ke CF

更新日期：2007-07-01 00:00:00

abstract：AIM AND OBJECTIVE:4-Hydroxyphenylpyruvate dioxygenase (HPPD), converting phydroxyphenylpyruvate (HPPA) to homogentisate (HGA), is an important target for treating type I tyrosinemia and synthesizing novel herbicides due to its significant role in tyrosine catabolism. Hence, it is imperative to design novel HPPD inhibit...

journal_title：Combinatorial chemistry & high throughput screening

authors： Fu Y,Sun YN,Cao HF,Yi KH,Zhao LX,Li JZ,Ye F

更新日期：2017-01-01 00:00:00

abstract：:Accurate classification of instances depends on identification and removal of redundant features. Classification of data having high dimensionality is usually performed in conjunction with an appropriate feature selection method. Feature selection enables identification of the most informative feature subset from the ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Patil D,Raj R,Shingade P,Kulkarni B,Jayaraman VK

更新日期：2009-06-01 00:00:00

abstract：:Arylamine N-acetyltransferases (NATs) are a family of enzymes found in eukaryotes and prokaryotes. While the precise endogenous function of NAT remains unknown for most organisms, recent evidence has shown that the expression of human NAT1 is up-regulated in estrogen receptor positive breast cancer. Additionally, NAT ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Westwood IM,Kawamura A,Russell AJ,Sandy J,Davies SG,Sim E

更新日期：2011-02-01 00:00:00

abstract：AIM AND OBJECTIVE:Thiazol-2-imine derivatives are interested for their pharmaceutical and biologic activities. A literature survey reveals that there have been no any reports on the synthesis of thiazol-2-imine derivatives without substituents in position C-4 and C-5 via one-pot reaction. Herein we report an efficient ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Nasiri F,Sabahi-Agabager L

更新日期：2017-01-01 00:00:00

abstract：:Time-resolved fluorescence (TRF) assay formats are frequently used technologies in high-throughput screening. In this article, we have characterised the novel Plate::Vision(2) 96-microlens array reader (Carl Zeiss Jena GmbH, Germany) and compared it to the novel LEADseeker Generation IV multimodality imaging system (L...

journal_title：Combinatorial chemistry & high throughput screening

authors： Merk S,Lietz A,Kroner M,Valler M,Heilker R

更新日期：2004-02-01 00:00:00

abstract：:High throughput screening (HTS) campaigns, where laboratory automation is used to expose biological targets to large numbers of materials from corporate compound collections, have become commonplace within the lead generation phase of pharmaceutical discovery. Advances in genomics and related fields have afforded a we...

journal_title：Combinatorial chemistry & high throughput screening

authors： Yang X,Parker D,Whitehead L,Ryder NS,Weidmann B,Stabile-Harris M,Kizer D,McKinnon M,Smellie A,Powers D

更新日期：2006-02-01 00:00:00

abstract：:The development of stents has been a major advancement over balloon angioplasty, improving vessel revascularization in obstructive coronary artery disease. The development of drug-eluting stents (DES) was the next breakthrough, designed to prevent the development of neointimal hyperplasia (restenosis) following percut...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hezi-Yamit A,Sullivan C,Wong J,David L,Chen M,Cheng P,Shumaker D,Wilcox J,Udipi K

更新日期：2009-08-01 00:00:00