Abstract：
:A set of chemically engineered extracts enriched in compounds including N-N and N-O fragments in their structures was prepared. Bromodomain binding screening and bioguided fractionation led to the identification of one oxime hit that interacts with TcBDF3 with affinity in the submicromolar range and that shows interesting antiparasitic properties against the different life cycle stages of T. cruzi.
journal_name
ACS Comb Scijournal_title
ACS combinatorial scienceauthors
Ramallo IA,Alonso VL,Rua F,Serra E,Furlan RLEdoi
10.1021/acscombsci.7b00172subject
Has Abstractpub_date
2018-04-09 00:00:00pages
220-228issue
4eissn
2156-8952issn
2156-8944journal_volume
20pub_type
杂志文章abstract：:3-Substituted 4-quinolones were synthesized using a one-pot metal-free strategy in moderate to quantitative yields. Carried out in dimethylsulfoxide (DMSO) via a sequential addition of materials, the methodology is tolerant of a wide range of functional groups and applicable to library synthesis. ...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/co1000103
更新日期：2011-01-10 00:00:00
abstract：:A library of functionalized 3-(α-styryl)-benzo[b]thiophenes, endowed with a high level of molecular diversity, was efficiently synthesized by applying a synthetic sequence that allowed introduction of various substituents on aromatic A, B, and C-rings. The strategy developed involves the synthesis of 3-bromobenzo[b]th...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/co500115b
更新日期：2014-12-08 00:00:00
abstract：:This work presents the first use of yeast-displayed protein targets for screening mRNA-display libraries of cyclic and linear peptides. The WW domains of Yes-Associated Protein 1 (WW-YAP) and mitochondrial import receptor subunit TOM22 were adopted as protein targets. Yeast cells displaying WW-YAP or TOM22 were magnet...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.0c00171
更新日期：2020-12-14 00:00:00
abstract：:In this research, MgAl-CO32- nanolayered double hydroxide (NLDH) was synthesized through a facile coprecipitation method, followed by a hydrothermal treatment. The prepared NLDHs were used as a hydrophilic nanofiller for improving the performance of the PVDF-based ultrafiltration membranes. The main objective of this ...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.7b00046
更新日期：2017-07-10 00:00:00
abstract：:This is a report on the early years of combinatorial materials science and technology. High-throughput technologies (HTTs) are found in life- and materials-science laboratories. Although HTTs have long been the standard in life sciences in academia as well as in industry, HTTs in materials science have become the stan...
journal_title：ACS combinatorial science
pub_type： 历史文章,杂志文章,评审
doi：10.1021/acscombsci.8b00189
更新日期：2019-06-10 00:00:00
abstract：:A potentiometric Pb(II)-selective sensor was fabricated by a combinatorial screening of electrically conducting polysulfoaminoanthraquinone (PSA) nanoparticles as a solid ionophore, ion exchangers (oleic acid (OA) and NaTPB), plasticizers in a polyvinyl chloride (PVC) matrix, membrane thickness, inner filling ion spec...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/co400140g
更新日期：2014-03-10 00:00:00
abstract：:We have achieved an efficient solution-phase parallel synthesis of a library of natural piper-amide-like compounds from the bifunctional β-phosphono-N-hydroxy-succinimidyl ester intermediate. The primary important feature in our study is the construction of natural-product-like molecules through the adaptation of soph...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/co400003d
更新日期：2013-04-08 00:00:00
abstract：:A one-bead one-compound (OBOC) library of peptide-based imaging agents was developed where a 19F-containing moiety was added onto the N-terminus of octamer peptides through copper-free click chemistry prior to screening of the library. This created a library of complete imaging agents that was screened against CXCR4, ...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.9b00146
更新日期：2020-03-09 00:00:00
abstract：:The development of a scanning reactor for planar catalysts is presented here. With respect to other existing models, this reactor is able to scan catalysts even with low turnover frequencies with a minimum sensed circular area of approximately 6 mm in diameter. The downstream gas analysis is performed with a quaprupol...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.5b00103
更新日期：2016-01-11 00:00:00
abstract：:Adleman's illustration of molecular computing using DNA paved the way toward an entirely new direction of computing (Adleman, L. M. Science 1994, 266, 1021). The exponential time complex combinatorial problem on a traditional computer turns out to be a separation problem involving a polynomial number of steps in DNA c...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.9b00150
更新日期：2020-05-11 00:00:00
abstract：:Copolymerization of isoprene (IP) with glycidyl methacrylate (GMA) was performed under RAFT (reversible addition-fragmentation chain-transfer) polymerization conditions in a platform for high-output experimentation. Covering the range between 1 and 0.2 molar fraction of IP in the feed, four sets of reactions were carr...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.9b00110
更新日期：2019-12-09 00:00:00
abstract：:In this article, an original one-pot method is utilized to synthesize a variety of derivatives of naphtho[2,1-b]furan-2(1H)-one via a pseudo-four-component domino reaction of aryl aldehydes, acetic anhydride, hippuric acids, and 2-naphthols catalyzed by HSW@SPIONs. This reaction illustrates an array of attractive feat...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.5b00018
更新日期：2015-08-10 00:00:00
abstract：:The Au-Al alloy system was investigated via a combinatorial thin film sputtering method for its potential as a plasmonic material. Au xAl1- x combinatorial libraries were cosputtered from Au and Al elemental targets and the composition, phase, and dielectric function of a ∼350 nm film was determined using energy dispe...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.8b00091
更新日期：2018-11-12 00:00:00
abstract：:For a future structure-activity relationship (SAR) study, a library of desketoraloxifene analogues has been prepared by parallel synthesis using iodocyclization and subsequent palladium-catalyzed coupling reactions. Points of desketoraloxifene diversification involve the two phenolic hydroxyl groups and the aliphatic ...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/co200090p
更新日期：2011-09-12 00:00:00
abstract：:A condition-based skeletal divergent synthesis was explored to achieve skeletal diversity in two component condensation reaction. Cyanomethyl benzimidazole was reacted with α-bromoketone under thermal conditions to furnish 2-aminofuranyl-benzimidazoles, while the same reaction afforded 3-cyano-benzopyrrolo-imidazoles ...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.7b00052
更新日期：2017-07-10 00:00:00
abstract：:High-throughput calculations can be applied to a large number of compounds, in order to discover new useful materials. In the present work, ternary intermetallic compounds are investigated, to find new potentially interesting materials for thermoelectric applications. The screening of stable nonmetallic compounds requ...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.0c00133
更新日期：2020-12-14 00:00:00
abstract：:High-throughput experimentation provides efficient mapping of composition-property relationships, and its implementation for the discovery of optical materials enables advancements in solar energy and other technologies. In a high throughput pipeline, automated data processing algorithms are often required to match ex...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.6b00053
更新日期：2016-11-14 00:00:00
abstract：:One-pot and efficient syntheses of structurally diverse isoquinolin-3-ones and isoquinolin-3-one-based benzo-1,4-diazepin-2,5-diones have been developed. The notable features of the process include the Ugi condensation of monomasked phthalaldehydes with amines, carboxylic acids, and isonitriles, followed by HClO4-medi...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/co400001h
更新日期：2013-04-08 00:00:00
abstract：:Metal-organic frameworks (MOFs) are nanoporous materials with exceptional host-guest properties poised for groundbreaking innovations in gas separation applications according to high-throughput (HT) screening data. However, MOF structural libraries are nearly infinite in practice and so statistical and information tec...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.5b00188
更新日期：2016-05-09 00:00:00
abstract：:In view of the variety and complexity of thermoelectric (TE) material systems, combinatorial approaches to materials development come to the fore for identifying new promising compounds. The success of this approach is related to the availability and reliability of high-throughput characterization methods for identify...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.7b00019
更新日期：2018-01-08 00:00:00
abstract：:Cr-Al-N thin film materials libraries were synthesized by combinatorial reactive high power impulse magnetron sputtering (HiPIMS). Different HiPIMS repetition frequencies and peak power densities were applied altering the ion to growth flux ratio. Moreover, time-resolved ion energy distribution functions were measured...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.9b00123
更新日期：2019-12-09 00:00:00
abstract：:Unfunctionalized alkylbiphenyls were fabricated by a parallel and combinatorial synthesis using pentaerythritol as a tetrapodal soluble support for a sulfonate-based traceless multifunctional linker system. Nickel N-heterocyclic carbene-catalyzed reactions of pentaerythritol tetrakis(biphenylsulfonate)s with primary a...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/co400136k
更新日期：2014-05-12 00:00:00
abstract：:A novel three-component, two-step, one-pot nucleophilic aromatic substitution (SNAr)-intramolecular cyclization-Suzuki coupling reaction was developed for the synthesis of benzo[h][1,6]naphthyridin-2(1H)-ones (Torins). On the basis of the new efficiently convergent synthetic route, a library of Torin analogs was synth...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.7b00119
更新日期：2017-12-11 00:00:00
abstract：:An efficient discovery strategy by combining diversity-oriented synthesis and converging cellular screening is described. By a three-round screening process, we identified novel tricyclic pyrido[2,3-b][1,4]benzothiazepines showing potent inhibitory activity against paclitaxel-resistant cell line H460TaxR (EC50 < 1.0 μ...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.6b00010
更新日期：2016-05-09 00:00:00
abstract：:We report the first example of venting-while-heating microwave-assisted synthesis of a small library of 3-arylthioindoles. Compounds were prepared in excellent isolated yields (90-98%) within 4 min in a closed vessel by treating indoles with disulfides in the presence of sodium hydride in anhydrous N,N-dimethylformami...
journal_title：ACS combinatorial science
pub_type： 信件
doi：10.1021/co200165j
更新日期：2012-04-09 00:00:00
abstract：:Parallel solution-phase synthesis of combinatorial libraries of dihydroindenoisoquinolines employing a sequential Cu(I)/Pd(0)-catalyzed multicomponent coupling and annulation protocol was realized. The scope and limitations of the protocol with respect to the substitution pattern in the aryl ring of the indene core, a...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/co200027c
更新日期：2011-09-12 00:00:00
abstract：:Retinoic acid (RA) is a key metabolite necessary for embryonic development and differentiation in vertebrates. We demonstrate the utility of genetically encoded, ligand-activatable single-chain bioluminescence probes for detecting RAs from different biological sources. We examined 13 different molecular designs to ide...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.9b00035
更新日期：2019-06-10 00:00:00
abstract：:The thin film system Ti-Ni-Si was investigated using methods of combinatorial materials science. A thin film composition spread library of the system was fabricated using combinatorial magnetron sputtering. The functional properties Seebeck coefficient, electrical resistivity, and luminance were determined using high-...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.8b00181
更新日期：2019-05-13 00:00:00
abstract：:Peptides are still difficult to synthesize when they contain sterically hindered amino acids, such as α,α-disubstituted amino acids and N-substituted amino acids. In this study, solid-phase syntheses of oligopeptides containing multiple α-aminoisobutyric acid (Aib) residues were performed in high yields by using a non...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/acscombsci.7b00184
更新日期：2018-03-12 00:00:00
abstract：:We report the parallel synthesis of a series of novel 4,9-dioxo-4,9-dihydro-1H-naphtho[2,3-d][1,2,3]triazol-3-ium chloride salts, which are analogs to cationic anthraquinones. Three synthetic protocols were examined leading to a convenient and facile library synthesis of the cationic anthraquinone analogs that contain...
journal_title：ACS combinatorial science
pub_type： 杂志文章
doi：10.1021/co2002075
更新日期：2012-03-12 00:00:00
