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：:Applications of silica-ROMP reagents in a one-pot, sequential protocol have been developed for the synthesis of a variety of diverse benzoxathiazepine 1,1-dioxides. This protocol includes sulfonylation, intramolecular SNAr, alkylation with silica-supported oligomeric benzyl (Si-OBPn) and triazole (Si-OTPn) phosphates,...

journal_title：ACS combinatorial science

authors： Faisal S,Maity PK,Zang Q,Samarakoon TB,Sourk RL,Hanson PR

更新日期：2016-07-11 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

authors： Xiang J,Zhang Z,Mu Y,Xu X,Guo S,Liu Y,Russo DP,Zhu H,Yan B,Bai X

更新日期：2016-05-09 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

authors： Fernandez M,Barnard AS

更新日期：2016-05-09 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

authors： Chen LH,Chung TW,Narhe BD,Sun CM

更新日期：2016-03-14 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：: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：:A Fe-Co-Nb thin film materials library was deposited by combinatorial magnetron sputtering and investigated by high-throughput methods to identify new noncubic ferromagnetic phases, indicating that combinatorial experimentation is an efficient method to discover new ferromagnetic phases adequate for permanent magnet a...

journal_title：ACS combinatorial science

authors： Alexandrakis V,Wallisch W,Hamann S,Varvaro G,Fidler J,Ludwig A

更新日期：2015-11-09 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：:A novel method of evaluating the enantioselectivity of chiral receptors is investigated. It involves extraction of an ionic guest in racemic form from an ion-exchange resin to the organic solvent, where it is bound by a chiral receptor. The enantioselectivity of the examined receptor is determined simply by measuring ...

journal_title：ACS combinatorial science

authors： Ulatowski F,Hamankiewicz P,Jurczak J

更新日期：2015-09-14 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

authors： Salami-Ranjbaran E,Khosropour AR,Mohammadpoor-Baltork I,Moghadam M,Tangestaninejad S,Mirkhani V

更新日期：2015-08-10 00:00:00

abstract：:A sequential single-flask multicomponent reactions is highly effective for the synthesis of 1,2-dihydroisoquinolines through amidealkylation from intermediate N-acylisoquinolinium salts under mild conditions. N-Acylisoquinolinium ions and trichloromethyl-1-(1H-indol-3-yl)isoquinoline-2(1H)-carboxylate have demonstrate...

journal_title：ACS combinatorial science

authors： Chung TW,Hung YT,Thikekar T,Paike VV,Lo FY,Tsai PH,Liang MC,Sun CM

更新日期：2015-08-10 00:00:00

abstract：:Protein-protein interactions are generally challenging to target by small molecules. To address the challenge, we have used a multidisciplinary approach to identify small-molecule disruptors of protein-protein interactions that are mediated by SUMO (small ubiquitin-like modifier) proteins. SUMO modifications have emer...

journal_title：ACS combinatorial science

authors： Alontaga AY,Li Y,Chen CH,Ma CT,Malany S,Key DE,Sergienko E,Sun Q,Whipple DA,Matharu DS,Li B,Vega R,Li YJ,Schoenen FJ,Blagg BS,Chung TD,Chen Y

更新日期：2015-04-13 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：:Solid-phase synthetic strategies toward the generation of libraries of biologically relevant molecules were developed using olefin cross-metathesis as a key step. It is remarkably the formal alkane metathesis based on a one-pot, microwave-assisted, ruthenium-catalyzed cross-metathesis and reduction to obtain Csp3-Csp3...

journal_title：ACS combinatorial science

authors： Méndez L,Mata EG

更新日期：2015-02-09 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

authors： Srivastava A,Aggarwal L,Jain N

更新日期：2015-01-12 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 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

authors： Tréguier B,Lawson M,Bernadat G,Bignon J,Dubois J,Brion JD,Alami M,Hamze A

更新日期：2014-12-08 00:00:00

abstract：:An expedient and metal-free synthetic protocol for construction of substituted quinolines has been developed from anilines and phenylacetaldehydes using imidazolium cation-based ionic liquids as the reaction medium. Mechanistic analysis indicated that the reaction occurs through C-C and C-N bond formation to produce i...

journal_title：ACS combinatorial science

authors： Bharate JB,Bharate SB,Vishwakarma RA

更新日期：2014-11-10 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：:The present investigation reports an easy access to a library of novel spiro-oxindole-pyrrolizine or pyrrolo[1,2-c]thiazole fused coumarin hybrid heterocycles through a one-pot sequential four-component reactions of 2,2-dimethyl-1,3-dioxane-4,6-dione, salicylaldehydes, isatins, and cyclic α-amino acids under ultrasoun...

journal_title：ACS combinatorial science

authors： Kanchithalaivan S,Sumesh RV,Kumar RR

更新日期：2014-10-13 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 series of diverse polycyclic heterocycles containing spirooxindole, pyridine/thiophene, and pyrrolidine/pyrrolizidine/pyrrolothiazole rings have been synthesized through the 1,3-dipolar cycloaddition of azomethine ylides generated in situ by the condensation of dicarbonyl compounds (isatin or acenaphthenequinone) an...

journal_title：ACS combinatorial science

authors： Li J,Wang J,Xu Z,Zhu S

更新日期：2014-09-08 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

authors： Xie YJ,Sun J,Yan CG

更新日期：2014-06-09 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：: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 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

authors： Postma TM,Albericio F

更新日期：2014-04-14 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

authors： Li Y,Xue Z,Ye W,Liu J,Yao J,Wang C

更新日期：2014-03-10 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

authors： Huang MR,Ding YB,Li XG

更新日期：2014-03-10 00:00:00

abstract：:A combinatorial library having 66 different ternary compositions of Pd-Ir-Ce was prepared via the impregnation method to find the optimum ternary composition with the highest performance toward oxygen reduction reaction (ORR) in acid media. Its performance in ORR activity of the combinatorial array was evaluated throu...

journal_title：ACS combinatorial science

authors： Park SH,Choi CH,Koh JK,Pak C,Jin SA,Woo SI

更新日期：2013-11-11 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

authors： Kim S,Lim C,Lee S,Lee S,Cho H,Lee JY,Shim DS,Park HD,Kim S

更新日期：2013-04-08 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：: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

authors： La Venia A,Dolenský B,Krchňák V

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

authors： Hazra A,Bharitkar YP,Chakraborty D,Mondal SK,Singal N,Mondal S,Maity A,Paira R,Banerjee S,Mondal NB

更新日期：2013-01-14 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：: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：:Functionalized chromenes have been synthesized via highly selective metal-free domino reactions from ketones and phenols. 2H-Chromenes, 4H-chromenes, spiran and benzocyclopentane can be respectively prepared starting from the corresponding cyclic ketones, aryl methyl ketones, acetone, and 3-pentanone. ...

journal_title：ACS combinatorial science

authors： Xue WJ,Li Q,Gao FF,Zhu YP,Wang JG,Zhang W,Wu AX

更新日期：2012-08-13 00:00:00

abstract：:Thirteen 5-hetarylaminopyrazoles were synthesized in 62-93% yield through the arylation of 1-isopropyl- and 1-phenyl-5-aminopyrazoles with electrophilic hetarylhalides under optimized conditions. Condensation of 5-hetarylaminopyrazoles with carbonyl compounds facilitated by AcOH or Me(3)SiCl furnished 23 pyrazolo[3,4-...

journal_title：ACS combinatorial science

authors： Ryabukhin SV,Granat DS,Plaskon AS,Shivanyuk AN,Tolmachev AA,Volovenko YM

更新日期：2012-08-13 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

authors： Talbot A,Maltais R,Poirier D

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

authors： Faisal S,Ullah F,Maity PK,Rolfe A,Samarakoon TB,Porubsky P,Neuenswander B,Lushington GH,Basha FZ,Organ MG,Hanson PR

更新日期：2012-04-09 00:00:00