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 nonswellable resin as the solid-support and 3-nitro-1,2,4-triazol-1-yl-tris(pyrrolidin-1-yl)phosphonium hexafluorophosphate (PyNTP) as the condensing reagent.
journal_name
ACS Comb Scijournal_title
ACS combinatorial scienceauthors
Hara RI,Mitsuhashi Y,Saito K,Maeda Y,Wada Tdoi
10.1021/acscombsci.7b00184subject
Has Abstractpub_date
2018-03-12 00:00:00pages
132-136issue
3eissn
2156-8952issn
2156-8944journal_volume
20pub_type
杂志文章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::Thin films of two types of high-entropy oxides (HEOs) have been deposited on 76.2 mm Si wafers using combinatorial sputter deposition. In one type of the oxides, (MgZnMnCoNi)O x , all the metals have a stable divalent oxidation state and similar cationic radii. In the second...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.0c00159
更新日期:2020-12-14 00:00:00
abstract::A novel parallel medicinal chemistry (PMC)-enabled synthesis of 1H-pyrazolo[3,4-d]pyrimidines employing condensation of easily accessible N-pyrazolylamides and nitriles has been developed. The presented studies describe singleton and library enablements that allowed rapid generation of molecular diversity to examine C...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.7b00116
更新日期:2017-11-13 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::An efficient and straightforward synthetic protocol has been developed for the diversity-oriented synthesis of highly functionalized piperidines containing a Meldrum's acid moiety via pseudo five-component reaction between aromatic aldehydes, ammonium acetate, substituted β-nitrostyrenes and Meldrum's acid for the gen...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co4001502
更新日期:2014-03-10 00:00:00
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::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::Individually, benzoxazole and triazole moieties are of significant biological interest owing to their importance in drugs and pharmaceuticals. To assess their combined biological impact when woven into one molecule, we designed a novel, regioselective, multicomponent, one-pot (MCOP) approach for the construction of be...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co500135z
更新日期:2015-01-12 00:00:00
abstract::A series of LiMn1-x-yFexVyPO4 (LMFVP) nanomaterials have been synthesized using a pilot-scale continuous hydrothermal synthesis process (CHFS) and evaluated as high voltage cathodes in Li-ion batteries at a production rate of 0.25 kg h-1. The rapid synthesis and screening approach has allowed the specific capacity of ...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.6b00035
更新日期:2016-11-14 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::A novel immobilized N-chlorosuccinimide resin was developed for peptide disulfide bond formation in combinatorial libraries. The resin is prepared in a simple two-step process from commercial starting materials. Disulfide formation is initiated by adding a peptide solution to the resin, and excess reagent is removed b...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co500003p
更新日期:2014-04-14 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::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::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::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::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::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::Ultrasound-assisted synthesis of benzimidazo[2,1-b]quinazolin-1(1H)-ones was achieved via piperidine-catalyzed three-component reaction of 2-aminobenzimidazoles, an aromatic aldehyde, and 1,3-dione in aqueous isopropanol. This mechanism was first suspected following our identification of unusual reaction intermediates...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.5b00186
更新日期:2016-03-14 00:00:00
abstract::Acetylenic tertiary alcohols are well-known to be compounds that are biologically more stable than their corresponding secondary alcohols. The linkage of an acetylenic compound to a polymer support and further introduction of molecular diversity was found to be an interesting way to generate libraries of hydroxy acety...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co300034y
更新日期:2012-06-11 00:00:00
abstract::A combination of MACOS scale-out and ROMP-derived oligomeric triazole phosphates (OTP(n)) have been successfully utilized for the preparation of a 106-member library of triazole containing benzothiaoxazepine-1,1-dioxides. This report demonstrates the utilization of a suite of soluble OTP(n) reagents for facile (triazo...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co2001839
更新日期:2012-04-09 00:00:00
abstract::Electromanipulation and electrical characterization of cancerous cells is becoming a topic of high interest as the results reported to date demonstrate a good differentiation among various types of cells from an electrical viewpoint. Dielectrophoresis and broadband dielectric spectroscopy are complementary tools for s...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.0c00109
更新日期:2020-11-09 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::A new one-pot, three component reaction involving the use of Julia reagent, aldehyde, and sodium azide was developed for the efficient synthesis of N-unsubstituted 1,2,3-triazoles. This reaction could be carried out under mild reaction conditions without any precaution, and broad scope of substrates, both respect to J...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co5001597
更新日期:2015-03-09 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::Magnetization using cheap and minimally toxic materials, such as iron oxide nanoparticles can enable easy separation of cells from culture medium and is relevant to several industrial applications. Here, we show that cell surface expression of a mutant protein that binds iron oxide can enable efficient magnetization o...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/acscombsci.8b00084
更新日期:2018-10-08 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::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::The reactions of vinyl malononitriles with 3-phenacylideneoxindoles in ethanol in the presence of DBU as base resulted in the functionalized spirocyclic oxindoles through the domino Michael addition and intramolecular nucleophilic addition to cyano group. On the other hand, the similar reaction in the presence of pipe...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co500006c
更新日期:2014-06-09 00:00:00
abstract::Polymer-supported N-(2-oxo-ethyl)-derivatized Ser/Thr/Cys-containing dipeptides were synthesized and subjected to acid-mediated tandem N-acylium ion cyclization-nucleophilic addition to yield tetrahydro-2H-oxazolo[3,2-a]pyrazin-5(3H)-ones. The reaction conditions and building-block combinations for stereoselective syn...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co3001567
更新日期:2013-03-11 00:00:00
abstract::Dispiro-pyrrolidino/pyrrolizidino fused oxindoles/acenaphthoquinones have been derived from andrographolide via azomethine ylide cycloaddition to the conjugated double-bond under microwave (MW) irradiation. The reactions are chemo-, stereo-, and regioselective in nature. Change in amino acid from sarcosine/N-benzyl gl...
journal_title:ACS combinatorial science
pub_type: 杂志文章
doi:10.1021/co3001154
更新日期:2013-01-14 00:00:00