The Novartis compound archive -- from concept to reality.

abstract：:Microwave-assisted Suzuki-Miyaura and Stille cross-coupling reactions for the synthesis of highly electron-rich and diversely functionalized biaryl intermediates are presented. Microwave-irradiation has been demonstrated to be a very powerful tool for performing difficult transition metal-catalyzed cross-coupling reac...

journal_title：Combinatorial chemistry & high throughput screening

authors： Appukkuttan P,Dehaen W,Van der Eycken E

更新日期：2007-11-01 00:00:00

abstract：:High Throughput experimentation has been well established as a tool in early stage catalyst development and catalyst and process scale-up today. One of the more challenging areas of catalytic research is polymer catalysis. The main difference with most non-polymer catalytic conversions is the fact that the product is ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Gruter GJ,Sipos L,Adrianus Dam M

更新日期：2012-02-01 00:00:00

abstract：:Artificial neural networks (ANNs) have been applied for the quantitative structure-activity relationships (QSAR) studies of antibacterial activity against Escherichia coli, Serratia marcescens, Proteus vulgaris, Klebsiella pneumoniae and Pseudomonas aeruginosa of a large series of new imidazole derivatives. Antibacter...

journal_title：Combinatorial chemistry & high throughput screening

authors： Bucinski A,Markuszewski MJ,Wiktorowicz W,Krysinski J,Kaliszan R

更新日期：2004-06-01 00:00:00

abstract：:Both a development of resistance to artemisinin monotherapy and lack of effective vaccine against malaria have created the urgent need for the development of new and efficient antimalarial agents. In this background, we have developed here a linear discriminant analysis (LDA) model and a few 3D-pharmacophore models fo...

journal_title：Combinatorial chemistry & high throughput screening

authors： Aher RB,Roy K

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND:Lead (Pb) remains a common contaminant in the environment in many parts of the world. Pb exposure adversely affects many human organs, including the gonads, via oxidant and inflammatory marker propagation in affected tissues. Moringa oleifera leaf extract (MOE) is a rich source of antioxidants reported to ha...

journal_title：Combinatorial chemistry & high throughput screening

authors： Albasher G,Alrajhi R,Alshammry E,Almeer R

更新日期：2020-09-23 00:00:00

abstract：:The high level of attrition of drugs in clinical development has led pharmaceutical companies to increase the efficiency of their lead identification and development through techniques such as combinatorial chemistry and high-throughput (HTP) screening. Since the major reasons for clinical drug candidate failure other...

journal_title：Combinatorial chemistry & high throughput screening

authors： Shearer TW,Smith KS,Diaz D,Asher C,Ramirez J

更新日期：2005-02-01 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：:Cell surfaces, especially mammalian cell surfaces, are heavily coated with complex poly- and oligosaccharides, and these glycans have been implicated in many functions, such as cell-to-cell communication, host-pathogen interactions and cell matrix interactions. Not surprisingly then, the aberrations of glycosylation a...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zhou SM,Cheng L,Guo SJ,Zhu H,Tao SC

更新日期：2011-09-01 00:00:00

abstract：OBJECTIVE:The aim of this study areto screen MicroRNAs (miRNAs) related to the prognosis of lung adenocarcinoma (LUAD) and to explore the possible molecular mechanisms. METHODS:The data for a total of 535 patients with LUAD data were downloaded from The Cancer Genome Atlas (TCGA) database. The miRNAs for LUAD prognosi...

journal_title：Combinatorial chemistry & high throughput screening

authors： Wang W,Liu B,Duan X,Feng X,Wang T,Wang P,Ding M,Zhang Q,Feng F,Wu Y,Yao W,Wang Q,Yang Y

更新日期：2020-01-01 00:00:00

abstract：:Polo-like kinase 1 (Plk1) is a decisive enzyme with its multifunctional activity in cell cycle progression especially mitosis. The over expression of Plk1 in broad spectrum of cancer types turns into a promising therapeutic target against cancer. In the present study, several ligand based pharmacophore models and atom...

journal_title：Combinatorial chemistry & high throughput screening

authors： Chekkara R,Gorla VR,Susithra E,Tenkayala SR

更新日期：2014-01-01 00:00:00

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 woul...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ladyman MK,Walton JG,Lilienkampf A,Bradley M

更新日期：2016-01-01 00:00:00

abstract：:In this review various technologies and approaches for the utilization of mass spectrometry in high-throughput analyses are discussed. The use of quadrupole-based mass spectrometry in the screening of chemical libraries against enzymatic targets for the identification of inhibitors and/or activators is highlighted. Th...

journal_title：Combinatorial chemistry & high throughput screening

authors： Jonas M,LaMarr WA,Ozbal C

更新日期：2009-09-01 00:00:00

abstract：AIM:It has been reported that glial cells are involved in Alzheimer's disease (AD). According to our previous research, Scutellaria barbata flavonoids (SBFs) can protect the neuronal disorder and memory impairment for AD-like rats, while the effect of SBFs on the glial cells disorder in AD-like rats has been less well ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Cheng JJ,Guo Q,Wu XG,Ma S,Gao Y,Ya-Zhen S

更新日期：2020-12-08 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

authors： Zhu J,Li Y,Yu H,Zhang L,Mao X,Hou T

更新日期：2012-07-01 00:00:00

abstract：AIM AND OBJECTIVE:To determine the mechanisms present in the etiopathogenesis of nasal polyposis. It is not clear whether amino acids contribute in a causal way to the development of the disease. Therefore, the aim of this study was to determine the plasma-free amino acid profile in patients with nasal polyposis and to...

journal_title：Combinatorial chemistry & high throughput screening

authors： Celik M,Şen A,Koyuncu İ,Gönel A

更新日期：2019-01-01 00:00:00

abstract：:Shotgun phage display cloning is a useful tool for studying interactions between bacterial and host proteins. Libraries are constructed by cloning randomly fragmented prokaryotic DNA into phage mid-vectors. Theoretically, these libraries will consist of phages that together display all proteins encoded by the bacteria...

journal_title：Combinatorial chemistry & high throughput screening

authors： Jacobsson K,Frykberg L

更新日期：2001-04-01 00:00:00

abstract：:Whole Cell-matrix-assisted laser desorption/ionization-time-of-flight mass spectrometry (MALDI-TOF-MS) is an emerging sensitive technique for rapid typing of microorganisms, efficient screening of biocombinatorial libraries of natural compounds and the analysis of complex biological samples, as whole cells, subcellula...

journal_title：Combinatorial chemistry & high throughput screening

authors： Vater J,Gao X,Hitzeroth G,Wilde C,Franke P

更新日期：2003-09-01 00:00:00

abstract：:Natural products obtained from marine sources are considered to be a rich and diverse source of potential drugs. In the present work we demonstrate the use of chemoinformatics approach for the design of new molecules inspired by molecules from marine organisms. Accordingly we have assimilated information from two majo...

journal_title：Combinatorial chemistry & high throughput screening

authors： Karthikeyan M,Nimje D,Pahujani R,Tyagi K,Bapat S,Vyas R,Pillai Padmakumar K

更新日期：2015-01-01 00:00:00

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

authors： Nikolic D,Fan PW,Bolton JL,van Breemen RB

更新日期：1999-06-01 00:00:00

abstract：:The Nobel Prize in Chemistry 1902 was given to Hermann Emil Fischer "in recognition of the extraordinary services he had rendered by his work on sugar and purine synthesis". This truly great chemist of all time named a group of bicyclic nitrogenous structures as purines, discovered the synthesis of glucose, fructose a...

journal_title：Combinatorial chemistry & high throughput screening

authors： Franzén R,Tois J

更新日期：2003-08-01 00:00:00

abstract：:Approximately 5-10% of all colorectal carcinomas arise from cancer predisposition syndromes caused by heterozygote germline mutations in post-replicative DNA mismatch repair (MMR) genes. In contrast to gastrointestinal polyposis syndromes, carcinomas in these patients do not occur on the background of increased number...

journal_title：Combinatorial chemistry & high throughput screening

authors： Merkelbach-Bruse S,Köse S,Losen I,Bosserhoff AK,Buettner R

更新日期：2000-12-01 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

authors： Yu W,Wu X,Ren J,Zhang X,Wang Y,Li C,Xu W,Li J,Li G,Zheng W,Liao H,Yuan X

更新日期：2020-10-26 00:00:00

abstract：:The identification of clones expressing high levels of recombinant protein in Pichia pastoris is usually dependant upon SDS-PAGE, Western blotting, or bioactivity-based assays that are labour and time-consuming. We describe a rapid method that images green fluorescence protein (GFP) of individual P. pastoris clones tr...

journal_title：Combinatorial chemistry & high throughput screening

authors： Al-Samarrai TH,Kirk CA,Jones WT,Harvey D,Templeton MD

更新日期：2010-06-01 00:00:00

abstract：:Drug metabolism can have profound effects on the pharmacological and toxicological profile of therapeutic agents. In the pharmaceutical industry, many in vitro techniques are in place or under development to screen and optimize compounds for favorable metabolic properties in the drug discovery phase. These in vitro te...

journal_title：Combinatorial chemistry & high throughput screening

authors： Masimirembwa CM,Thompson R,Andersson TB

更新日期：2001-05-01 00:00:00

abstract：:The important factor which differentiates gemini surfactants from conventional monomeric surfactants is the spacer group. The molecular connectivity method was used to study the effect of the spacer group on critical micelle concentration of cationic gemini surfactants. Two models were derived employing only Kier and ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Mozrzymas A

更新日期：2016-01-01 00:00:00

abstract：:Recyclable ZnO nano-rods catalyst as a most efficient and straightforward protocol for one-pot, three-component synthesis of spirooxindole derivatives at room temperature under solvent-free conditions in both reaction media and work-up procedure is described. This method is of great value because of its environmentall...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hosseini-Sarvari M,Tavakolian M

更新日期：2012-12-01 00:00:00

abstract：:Combinatorial phage peptide libraries have been used to identify the ligands for specific target molecules. These libraries are also useful for identification of the specific substrates of various proteases. A substrate phage library has a random peptide sequence at the N-terminus of the phage coat protein and an addi...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ohkubo S,Miyadera K,Sugimoto Y,Matsuo K,Wierzba K,Yamada Y

更新日期：2001-11-01 00:00:00

abstract：:Calcium (Ca(2+)) fluoroionophores are useful in cell-based functional assays of G-protein coupled receptor (GPCR) activation or ion channel modulation. In this paper we describe new calcium probes that improve or overcome certain deficiencies in existing probes. These new fluoroionophores are based on acylation of ami...

journal_title：Combinatorial chemistry & high throughput screening

authors： Gee KR,Rukavishnikov A,Rothe A

更新日期：2003-06-01 00:00:00

abstract：:For years, the physicochemical properties of drug candidates have been used to predict their in vivo pharmacokinetic behaviors. Several theories and empirical correlations have been established by various researchers with the overall goal of expediting the drug candidate selection process, with greater confidence and ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Chiang PC,Hu Y

更新日期：2009-03-01 00:00:00

abstract：:Direct renin inhibitors (DRIs) have increasingly shown a significant advantage in the treatment of hypertension and protection of target organs. In this paper, a series of azaindole class renin inhibitors were subjected to 3D-QSAR study using Topomer CoMFA. Five kinds of splitting mode for different fragment cutting a...

journal_title：Combinatorial chemistry & high throughput screening

authors： Xiang Y,Song J,Zhang Z

更新日期：2014-01-01 00:00:00