Synthesis of a 3-(α-styryl)benzo[b]-thiophene library via bromocyclization of alkynes and palladium-catalyzed to sylhydrazones cross-couplings: evaluation as antitubulin agents.

abstract：:The extracellular-related kinase 5 (ERK5) is a promising target for cancer therapy. A high-throughput screen was developed for ERK5, based on the IMAP FP progressive binding system, and used to identify hits from a library of 57 617 compounds. Four distinct chemical series were evident within the screening hits. Resyn...

journal_title：ACS combinatorial science

authors： Myers SM,Bawn RH,Bisset LC,Blackburn TJ,Cottyn B,Molyneux L,Wong AC,Cano C,Clegg W,Harrington RW,Leung H,Rigoreau L,Vidot S,Golding BT,Griffin RJ,Hammonds T,Newell DR,Hardcastle IR

更新日期：2016-08-08 00:00:00

abstract：:A three-component reaction of a 2-aminoazine, a 2-oxoaldehyde, and a cyclic 1,3-dicarbonyl compound providing access toward a novel class of imidazo[1,2-a]azine derivatives was developed and studied. The scope of the process was thoroughly explored under three different reaction conditions resulting in the generation ...

journal_title：ACS combinatorial science

authors： Peshkov VA,Peshkov AA,Pereshivko OP,Van Hecke K,Zamigaylo LL,Van der Eycken EV,Gorobets NY

更新日期：2014-10-13 00:00:00

abstract：:A one-pot parallel synthesis of N(1)-aryl-N(2)-alkyl-substituted oxamides with 2,2,2-trifluoroethyl chlorooxoacetate was developed. The synthesis of a library of 45 oxamides revealed higher efficiency of this reagent over the known ethyl chlorooxoacetate. The reagent was successfully used to prepare the known oxamide-...

journal_title：ACS combinatorial science

authors： Bogolubsky AV,Moroz YS,Mykhailiuk PK,Pipko SE,Zhemera AV,Konovets AI,Stepaniuk OO,Myronchuk IS,Dmytriv YV,Doroschuk RA,Zaporozhets OA,Tolmachev A

更新日期：2015-10-12 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

authors： Nguyen TX,Su YH,Hattrick-Simpers J,Joress H,Nagata T,Chang KS,Sarker S,Mehta A,Ting JM

更新日期：2020-12-14 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

authors： Cruz-Teran CA,Bacon K,McArthur N,Rao BM

更新日期：2018-10-08 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

authors： Maier WF

更新日期：2019-06-10 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

authors： Shah AA,Chenard LK,Tucker JW,Helal CJ

更新日期：2017-11-13 00:00:00

abstract：:The possibility of band gap engineering in graphene opens countless new opportunities for application in nanoelectronics. In this work, the energy gaps of 622 computationally optimized graphene nanoflakes were mapped to topological autocorrelation vectors using machine learning techniques. Machine learning modeling re...

journal_title：ACS combinatorial science

authors： Fernandez M,Abreu JI,Shi H,Barnard AS

更新日期：2016-11-14 00:00:00

abstract：:A copper-catalyzed efficient one step three component strategy for preparing a library of aminoindolizino[8,7-b]indoles from N-substituted 1-formyl-9H-β-carbolines, secondary amines, and substituted alkynes with high atom economy has been developed. ...

journal_title：ACS combinatorial science

authors： Dighe SU,Hutait S,Batra S

更新日期：2012-12-10 00:00:00

abstract：:An efficient, three-component strategy for the improved synthesis of multifunctionalized 6,7-dihydrobenzofuran-4(5H)-ones under microwave irradiation in ethyl alcohol within short periods has been established. The synthesized benzofuran-4(5H)-ones have been readily converted into polyfunctionalized cinnoline-4-carboxa...

journal_title：ACS combinatorial science

authors： Ma GH,Tu XJ,Ning Y,Jiang B,Tu SJ

更新日期：2014-06-09 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

authors： Wambach M,Ziolkowski P,Müller E,Ludwig A

更新日期：2019-05-13 00:00:00

abstract：:Combinatorial synthesis of Li-ion batteries has proven extremely powerful in screening complex compositional spaces for next-generation materials. To date, no Na-ion counterpart exists wherein Na-ion cathodes can be synthesized in such a way to be comparable to that obtained in bulk synthesis. Herein, we develop a syn...

journal_title：ACS combinatorial science

authors： Adhikari T,Hebert A,Adamič M,Yao J,Potts K,McCalla E

更新日期：2020-06-08 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

authors： Kim WK,Jang JH,Jo H,Park K

更新日期：2014-05-12 00:00:00

abstract：:A sequential one-pot, two-step, three-component reaction for efficient synthesis of spiro-substituted 1,3-thiazine library has been developed. The syntheses were achieved by reacting cyanoacetamide with isothiocyanate derivatives to give rise to 2-cyano-3-mercaptoacrylamides, which are trapped in situ by various cyclo...

journal_title：ACS combinatorial science

authors： Zhuang QY,Wang X,Gao Y,Shi F,Jiang B,Tu SJ

更新日期：2011-01-10 00:00:00

abstract：:High-throughput combinatorial methods have been useful in identifying new oxide semiconductors with the potential to be applied to solar water splitting. Most of these techniques have been limited to producing and screening oxide phases formed at temperatures below approximately 550 °C. We report the development of a ...

journal_title：ACS combinatorial science

authors： Skorupska K,Maggard PA,Eichberger R,Schwarzburg K,Shahbazi P,Zoellner B,Parkinson BA

更新日期：2015-12-14 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

authors： Cho CH,Jung DI,Neuenswander B,Larock RC

更新日期：2011-09-12 00:00:00

abstract：:A microgradient-heater (MGH) was developed, and its feasibility as a tool for high-throughput materials science experimentation was tested. The MGH is derived from microhot plate (MHP) systems and allows combinatorial thermal processing on the micronano scale. The temperature gradient is adjustable by the substrate ma...

journal_title：ACS combinatorial science

authors： Meyer R,Hamann S,Ehmann M,Thienhaus S,Jaeger S,Thiede T,Devi A,Fischer RA,Ludwig A

更新日期：2012-10-08 00:00:00

abstract：:DNA-encoded synthesis is rekindling interest in combinatorial compound libraries for drug discovery and in technology for automated and quantitative library screening. Here, we disclose a microfluidic circuit that enables functional screens of DNA-encoded compound beads. The device carries out library bead distributio...

journal_title：ACS combinatorial science

authors： MacConnell AB,Price AK,Paegel BM

更新日期：2017-03-13 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

authors： Marelli M,Nemenyi A,Dal Santo V,Psaro R,Ostinelli L,Monticelli D,Dossi C,Recchia S

更新日期：2016-01-11 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

authors： Che C,Li S,Yu Z,Li F,Xin S,Zhou L,Lin S,Yang Z

更新日期：2013-04-08 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

authors： Barreteau C,Crivello JC,Joubert JM,Alleno E

更新日期：2020-12-14 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

authors： Chai H,Guo R,Yin W,Cheng L,Liu R,Chu C

更新日期：2015-03-09 00:00:00

abstract：:An efficient method is described for the solid-supported synthesis of imidazo[4,5-b]pyridines and imidazo[4,5-c]pyridines from 2,4-dichloro-3-nitropyridine. The key pyridine building block was reacted with polymer-supported amines, followed by replacement of the second chlorine with amines, nitro group reduction, and ...

journal_title：ACS combinatorial science

authors： Lemrová B,Smyslová P,Popa I,Oždian T,Zajdel P,Soural M

更新日期：2014-10-13 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

authors： Banko L,Ries S,Grochla D,Arghavani M,Salomon S,Pfetzing-Micklich J,Kostka A,Rogalla D,Schulze J,Awakowicz P,Ludwig A

更新日期：2019-12-09 00:00:00

abstract：:A build/couple/pair strategy for the synthesis of complex and densely functionalized small molecules is presented. The strategy relies on synthetically tractable building blocks (build), that is, diversely substituted hydrazides, α-hydroxy aldehydes, and boronic acids, which undergo Petasis 3-component reactions (coup...

journal_title：ACS combinatorial science

authors： Flagstad T,Hansen MR,Le Quement ST,Givskov M,Nielsen TE

更新日期：2015-01-12 00:00:00

abstract：:A combination of flow and batch chemistries has been successfully applied to the assembly of a series of trisubstituted drug-like pyrrolidines. This study demonstrates the efficient preparation of a focused library of these pharmaceutically important structures using microreactor technologies, as well as classical par...

journal_title：ACS combinatorial science

authors： Baumann M,Baxendale IR,Kuratli C,Ley SV,Martin RE,Schneider J

更新日期：2011-07-11 00:00:00

abstract：:Solid-phase synthesis is the method of choice for peptide preparation in both research and industrial settings. The whole synthetic process is governed by the initial functionalization of the resin. Although the literature provides several methods to determine such functionalization, the addition of an Fmoc-amino acid...

journal_title：ACS combinatorial science

authors： Al Musaimi O,Basso A,de la Torre BG,Albericio F

更新日期：2019-11-11 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

authors： Li H,Sun W,Huang X,Lu X,Patel PR,Kim M,Orr MJ,Fisher RM,Tanaka TQ,McKew JC,Simeonov A,Sanderson PE,Zheng W,Williamson KC,Huang W

更新日期：2017-12-11 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

authors： Johnson ID,Loveridge M,Bhagat R,Darr JA

更新日期：2016-11-14 00:00:00

abstract：:A high throughput combinatorial synthesis utilizing inkjet printing of precursor inks was used to rapidly evaluate Bi-alloying into double perovskite oxides for enhanced visible light absorption. The fast visual screening of photo image scans of the library plates identifies 4-metal oxide compositions displaying an in...

journal_title：ACS combinatorial science

authors： Newhouse PF,Zhou L,Umehara M,Boyd DA,Soedarmadji E,Haber JA,Gregoire JM

更新日期：2020-12-14 00:00:00