Resisting the Resistance in Cancer: Cheminformatics Studies on Short- Path Base Excision Repair Pathway Antagonists Using Supervised Learning Approaches.

abstract：:Herein, we describe a simple, four-step process for the preparation of 1,2,3-triazino[1,6- a]quinazolin-13-ones. This method involves ring-opening, quinazoline-forming condensation, reduction, diazotization accompanied by rapid intramolecular cyclization in the last step afforded the desired products with structurally...

journal_title：Combinatorial chemistry & high throughput screening

authors： Sayahi MH,Baghersaei S,Goli F,Moghimi S,Mahdavi M,Firoozpour L,Shafiee A,Foroumadi A

更新日期：2016-01-01 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：: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：:Chromatographic fingerprinting technique of traditional Chinese medicine (TCM) has proved to be a comprehensive strategy for assessing the intact quality of herbal medicine. In general, one could use the chromatographic techniques to obtain a relatively complete picture of herbal medicines, which are in common called ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Liang YZ,Xie PS,Chan K

更新日期：2010-12-01 00:00:00

abstract：:Gelatinase B/MMP-9 fulfills crucial regulator or effector functions in disease states and may be pharmacologically targeted by specific inhibitors. The characteristics of cleavages of a natural gelatinase B substrate were simulated and amino acids with zinc-ion chelating side-groups were employed to design a library o...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hu J,Dubois V,Chaltin P,Fiten P,Dillen C,Van den Steen PE,Opdenakker G

更新日期：2006-09-01 00:00:00

abstract：BACKGROUND:ADAMTS (A disintegrin-like metalloproteinase with thrombospondin motifs) is a group of 19 zinc-dependent metalloproteases known to function in many pathological and physiological processes, such as adhesion, cell fusion, signaling, proteolysis and ECM degradation. OBJECTIVES:The aim of this study was to dem...

journal_title：Combinatorial chemistry & high throughput screening

authors： Tayman MA,Koyuncu İ,Köklü NÖ

更新日期：2020-01-01 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：: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

authors： Huth JR,Sun C

更新日期：2002-12-01 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：:An efficient, one-pot and three-component synthesis of biologically important heterocyclic compounds is described from the reaction of primary amines and phenyl isothiocyanate in the presence of acryloyl chloride at room temperature without the need to use any catalyst. ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zolali A,Nasiri F,Omid-Niakan S

更新日期：2014-01-01 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：:Two approaches were utilized to increase the throughput of pulsed ultrafiltration assays of ligand binding to human serum albumin, reducing the volume of the ultrafiltration chamber and combining pulsed ultrafiltration with high performance liquid chromatography-atmospheric pressure chemical ionization mass spectromet...

journal_title：Combinatorial chemistry & high throughput screening

authors： Gu C,Nikolic D,Lai J,Xu X,van Breemen RB

更新日期：1999-12-01 00:00:00

abstract：:We have developed high throughput fluorescence cell imaging methods to screen chemical libraries for compounds with effects on diverse aspects of cell physiology. We describe screens for compounds that arrest cells in mitosis, that block cell migration, and that block the secretory pathway. Each of these screens yield...

journal_title：Combinatorial chemistry & high throughput screening

authors： Yarrow JC,Feng Y,Perlman ZE,Kirchhausen T,Mitchison TJ

更新日期：2003-06-01 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

authors： Phougat N,Khatri S,Singh A,Dangi M,Kumar M,Dabur R,Chhillar AK

更新日期：2014-01-01 00:00:00

abstract：AIM AND OBJECTIVE:In this work, we synthesized and characterized a novel Brönsted acidic ionic liquid from the reaction of N, N, N', N'-tetramethylethylenediamine with chlorosulfonic acid and explored its catalytic activity in 1, 8-dioxo-octahydroxanthenes synthesis. MATERIALS AND METHODS:Dimedone, aryl aldehydes, and...

journal_title：Combinatorial chemistry & high throughput screening

authors： Piralghar ZA,Hashemi MM,Ezabadi A

更新日期：2018-01-01 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：: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

authors： Adler A,Forster N,Homann M,Göringer HU

更新日期：2008-01-01 00:00:00

abstract：:Substructural Molecular Fragments (SMF) method was applied for computer-aided design of new compounds potentially possessing high anti-HIV activities: tetrahydroimidazobenzodiazepinone (TIBO) derivatives and 1-[2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) derivatives. Using available experimental data, the SMF...

journal_title：Combinatorial chemistry & high throughput screening

authors： Varnek A,Solov'ev VP

更新日期：2005-08-01 00:00:00

abstract：:EGFR (ErbB-1/HER1) kinase plays an important role in cancer therapy. Two classification models were established to predict whether a compound is an inhibitor or a decoy of human EGFR (ErbR-1) by using Kohonen's self-organizing map (SOM) and support vector machine (SVM). A dataset containing 1248 ATP binding site inhib...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kong Y,Qu D,Chen X,Gong YN,Yan A

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND:Corona Virus Disease 2019 (COVID-19) pandemic threatens patients, societies and healthcare systems around the world. There is an emergent need to search for possible medications. OBJECTIVE:This article intends to use virtual screening and molecular docking methods to find potential inhibitors that can respo...

journal_title：Combinatorial chemistry & high throughput screening

authors： Chtita S,Belhassan A,Aouidate A,Belaidi S,Bouachrine M,Lakhlifi T

更新日期：2020-07-30 00:00:00

abstract：:The evaluation of the relationships between the hormones involved in the urogenital tract cancer, including bladder, kidney, prostate, and testis, could prove important from diagnostic point of view. The determination of the steroid hormone profiles may likely provide a biomarker for discrimination of hormone-related ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Konieczna L,Belka M,Baczek T,Ruszkowski M,Struck W,Markuszewski M,Kaliszan R,Markuszewski M

更新日期：2013-07-01 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：:As technologies for high throughput and high content screening continue to evolve, new platforms for quantitative cellular imaging will play an increasingly important role in identifying and profiling lead compounds. To gain insight into the effects of a compound on cell morphology or intracellular events, it is neces...

journal_title：Combinatorial chemistry & high throughput screening

authors： Elliott GS

更新日期：2009-11-01 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：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：:We describe a high-throughput, quantitative technology for fast identification of all different clones present in selectively enriched phage surface-displayed cDNA libraries. The strategy is based on a combination of phage display and high-density arrays. To demonstrate the utility of the method cDNAs of Aspergillus f...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kodzius R,Rhyner C,Konthur Z,Buczek D,Lehrach H,Walter G,Crameri R

更新日期：2003-03-01 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：:Voltage-clamp techniques are typically used to study the plasma membrane proteins, such as ion channels and transporters that control bioelectrical signals. Many of these proteins have been cloned and can now be studied as potential targets for drug development. The two approaches most commonly used for heterologous e...

journal_title：Combinatorial chemistry & high throughput screening

authors： Papke RL,Smith-Maxwell C

更新日期：2009-01-01 00:00:00

abstract：BACKGROUND:Traditionally, Phragmitis rhizoma has been prescribed to relive a fever, vomiting, dysuria, and constipation, and to promote secretion of fluids. In addition, recent studies have reported its efficacy as a diuretic and antiemetic. Our previous study demonstrated that the Phragmitis rhizoma aqueous extract (E...

journal_title：Combinatorial chemistry & high throughput screening

authors： Shin S,Kim NS,Kim YA,Oh HR,Bang OS

更新日期：2019-08-08 00:00:00

abstract：:There is increasing evidence that redox regulation of transcription, particularly activator protein-1 (AP-1) and nuclear factor kappa B (NF-kappaB), is important in inflammatory diseases. Human thioredoxin (TRX), a member of the oxidoreductase superfamily, was initially identified, as a factor which augments the produ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Eguchi M,McMillan M,Nguyen C,Teo JL,Chi EY,Henderson WR Jr,Kahn M

更新日期：2003-11-01 00:00:00