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Qile Xu et al.
PloS one, 10(6), e0128710-e0128710 (2015-06-11)
A series of novel 3-alkyl-1,5-diaryl-1H-pyrazoles were synthesized as combretastatin A-4 (CA-4) analogues and evaluated for antiproliferative activity against three human cancer cell lines (SGC-7901, A549 and HT-1080). Most of the target compounds displayed moderate to potent antiproliferative activity, and 7k
Chun-Hao Chen et al.
Organic & biomolecular chemistry, 12(48), 9831-9836 (2014-10-31)
Selective synthesis of 1- and 3-substituted 2-methoxyindenes from the carboalkoxylations of 2-ethynylbenzyl ethers is described; the former is obtained efficiently with P(t-Bu)2(o-biphenyl)AuCl/NaBARF in DCM/MS 4 Å whereas the latter is produced preferably with P(t-Bu)2(o-biphenyl)AuCl/AgNTf2 in pre-dried DCM. Both 1- and
Yi Chen et al.
Chirality, 27(6), 392-396 (2015-05-13)
An improved and efficient synthesis of (+)-cloprostenol has been accomplished in nine steps and 26% overall yield from commercially available (-)-Corey lactone 4-phenylbenzoate alcohol . The present route avoids tedious purifications and requires only one column chromatography operation, which reduces
Bo Wu et al.
Nature communications, 6, 6468-6468 (2015-03-04)
The endohedral fullerenes lead to well-protected internal species by the fullerene cages, and even highly reactive radicals can be stabilized. However, the manipulation of the magnetic properties of these radicals from outside remains challenging. Here we report a system of
Isolation, identification and characterization of potential impurities in cabazitaxel and their formation.
Yongyi Wang et al.
Magnetic resonance in chemistry : MRC, 52(12), 783-788 (2014-08-16)
Victor R de la Rosa et al.
Organic & biomolecular chemistry, 13(10), 3048-3057 (2015-01-27)
A poly[(2-ethyl-2-oxazoline)-ran-(2-nonyl-2-oxazoline)] random copolymer was synthesized and its thermoresponsive behavior in aqueous solution modulated by the addition of different supramolecular host molecules. The macrocycles formed inclusion complexes with the nonyl aliphatic side-chains present in the copolymer, increasing its cloud point
Kun-Ming Jiang et al.
Medicinal chemistry (Shariqah (United Arab Emirates)), 11(5), 453-461 (2014-12-30)
A new series of (E)-N,2,3-triarylacrylamide derivatives were designed and synthesized as potent anticancer agents. Cytotoxicity of the 26 target compounds was evaluated in vitro against six cancer cell lines (HCT116, A549, MDA-MB-468, HepG2, SKNMC and SK-OV-3) by Sulforhodamine B colorimetric
Four new cembranoids from the soft coral Sarcophyton sp.
Zhong-Bin Cheng et al.
Magnetic resonance in chemistry : MRC, 52(9), 515-520 (2014-07-22)
Ho-Joong Kim et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 21(33), 11836-11842 (2015-07-07)
Threefold symmetric rigid-core molecules with an internally grafted poly(ethylene oxide) (PEO) chain were synthesized, and their self-assembled structures were characterized using differential scanning calorimetry, TEM, and 1D and 2D X-ray scatterings in the solid state. The tripod compounds based on
Andrea Gini et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 21(34), 12053-12060 (2015-07-28)
N-carbamoyl nitrones represent an important class of reagents for the synthesis of a variety of natural and biologically active compounds. These compounds are generally converted into valuable 4-isoxazolines upon cyclization reaction with dipolarophiles. However, these types of N-protected nitrones are
Loredana Leone et al.
ChemistryOpen, 4(3), 370-377 (2015-08-08)
Current molecular cryptography (MoCryp) systems are almost exclusively based on DNA chemistry and reports of cryptography technologies based on other less complex chemical systems are lacking. We describe herein, as proof of concept, the prototype of the first asymmetric MoCryp
Tatsuki Nakano et al.
Analytica chimica acta, 880, 145-151 (2015-06-21)
In this study, a novel pre-column excimer fluorescence derivatization reagent, 2-chloro-4-methoxy-6-(4-(pyren-4-yl)butoxy)-1,3,5-triazine (CMPT), was developed for polyamines, specifically histamine. By CMPT derivatization, the polyamines, histamine and tyramine were converted to polypyrene derivatives, and emitted intra-molecular excimer fluorescence at 475nm. This could
Krzysztof Lodarski et al.
Journal of enzyme inhibition and medicinal chemistry, 30(1), 98-106 (2014-03-29)
The study presents the discovery of novel butyrylcholinesterase (BuChE) inhibitors among derivatives of azaphenothiazines by application of in silico and in vitro screening methods. From an in-house library of compounds, 143 heterocyclic molecules derived from the azaphenothiazine scaffold were chosen
László Csaba Bencze et al.
Bioresource technology, 200, 853-860 (2015-11-23)
Carboxylated single-walled carbon nanotubes (SWCNTCOOH) were used as support for covalent immobilization of Candida antarctica lipase B (CaL-B) using linkers with different lengths. The obtained nanostructured biocatalysts with low diffusional limitation were tested in batch mode in the ethanolysis of
Francesco Russo et al.
ChemistryOpen, 4(3), 342-362 (2015-08-08)
This is the first report of 5-styryl-oxathiazol-2-ones as inhibitors of the Mycobacterium tuberculosis (Mtb) proteasome. As part of the study, the structure-activity relationship of oxathiazolones as Mtb proteasome inhibitors has been investigated. Furthermore, the prepared compounds displayed a good selectivity
Tuomas Mehtiö et al.
Carbohydrate research, 402, 102-110 (2014-12-17)
A series of copolyanhydrides, consisting of 2,3,4,5-tetra-O-acetylgalactaric acid (AGA) and adipic acid (AA) as monomer units, was polymerized. Synthesis of AGA monomer consisted of two steps. First, O-acetylation of galactaric acid secondary hydroxyl groups was performed using acetic anhydride as
Virsinha Reddy et al.
Organic & biomolecular chemistry, 13(12), 3732-3741 (2015-02-18)
An efficient and mild protocol for the direct construction of aryl- and alkyl-substituted isoquinolines has been realized through silver nitrate catalyzed aromatic annulation of o-(1-alkynyl)arylaldehydes and ketones with ammonium acetate. The salient feature of this methodology is that this annulation
Phuong Hoang Tran et al.
Molecules (Basel, Switzerland), 20(10), 19605-19619 (2015-10-31)
A fast and green method is developed for regioselective acylation of indoles in the 3-position without the need for protection of the NH position. The method is based on Friedel-Crafts acylation using acid anhydrides. The method has been optimized, and
Paulina Maksym-Bębenek et al.
Macromolecular bioscience, 15(11), 1616-1624 (2015-07-23)
The core-shell micelles in aqueous solutions were prepared at low CAC values (<0.1 mg · mL(-1) ) from amphiphilic graft copolymers consisting of poly(methyl methacrylate) backbone (120-165 units) with loosely grafted (17-40%) hydroxyl-capped PEG (9 vs 6 units in side chain) for drug
Tamara G M Treptow et al.
European journal of medicinal chemistry, 95, 552-562 (2015-04-12)
We described the first synthesis of fatty acid 3,4-dihydropyrimidinones (DHPM-fatty acids) using the Biginelli multicomponent reaction. Antiproliferative activity on two glioma cell lines (C6 rat and U-138-MG human) was also reported. The novel DHPM-fatty acids reduced glioma cell viability relative
Gianluca Gilardoni et al.
Chemistry & biodiversity, 12(6), 946-954 (2015-06-18)
Coussarea macrophylla (Mart.) Müll.Arg. (Rubiaceae) was collected in Ecuador, and the bark was extracted with AcOEt. Chromatographic separation afforded six novel 3,4-secocycloartane and 3,4-secodammarane triterpenes, named macrocoussaric acids A-F, together with the known metabolites secaubryenol and 3,4-secodammara-4(28),20,24-triene-3,26-dioic acid. The structures
Ryuji Uchida et al.
The Journal of antibiotics, 67(11), 777-781 (2014-06-12)
A small molecule named habiterpenol produced by actinomycete Phytohabitans suffuscus 3787_5 was found to abrogate bleomycin-induced G2 arrest in Jurkat cells. Habiterpenol showed no cytotoxic effect on Jurkat cells even at 273 μM; however, the compound inhibited bleomycin-induced G2 arrest in
Raj Kumar Roy et al.
Nature communications, 6, 7237-7237 (2015-05-27)
Biopolymers such as DNA store information in their chains using controlled sequences of monomers. Here we describe a non-natural information-containing macromolecule that can store and retrieve digital information. Monodisperse sequence-encoded poly(alkoxyamine amide)s were synthesized using an iterative strategy employing two
Safinaz E-S Abbas et al.
Chemical biology & drug design, 85(5), 608-622 (2014-10-17)
Four series of some 4-substituted-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine derivatives 5a-f, 6a-f, 8a-f, and 9a-f were designed to be screened for their antitumor activity. All compounds were evaluated against breast (MCF-7) and lung (A-549) cell lines. Six compounds 5a, 5b, 6b, 6e, 9e, and
Małgorzata Wierzbicka et al.
Photochemical & photobiological sciences : Official journal of the European Photochemistry Association and the European Society for Photobiology, 14(12), 2251-2260 (2015-11-05)
A series of symmetrically substituted diphenylbuta-1,3-diyne (DPB) derivatives possessing electron-donating (N,N-dimethylamino or methoxy) or electron-accepting (nitrile, ester or aldehyde) groups have been prepared and studied with emphasis on their spectral and photophysical properties. The photophysical characteristics of these compounds have
Yasuhiro Shimamoto et al.
Bioorganic & medicinal chemistry, 23(4), 876-890 (2015-01-24)
The design and evaluation of a novel decahydroisoquinolin scaffold as an inhibitor for severe acute respiratory syndrome (SARS) chymotrypsin-like protease (3CL(pro)) are described. Focusing on hydrophobic interactions at the S2 site, the decahydroisoquinolin scaffold was designed by connecting the P2
Bhakti B Salgaonkar et al.
International journal of biological macromolecules, 78, 339-346 (2015-04-22)
Polyhydroxyalkanoates (PHA's) can be a key solution for pollution problems caused by plastics derived from petrochemical sources. Extremely halophilic archaeon Halogeometricum borinquense strain E3 showed maximum PHA accumulation of 73.51 ±1.7% (wt/wt) of cell dry weight (CDW) with 2% glucose.
Vladimir E Oslovsky et al.
Nucleosides, nucleotides & nucleic acids, 34(7), 475-499 (2015-07-15)
Several methods for the preparation of some N(6)-substituted adenosines based on selective 1-N-alkylation with subsequent Dimroth rearrangement were developed. The proposed methods seem to be effective for the preparation of natural N(6)-isopentenyl- and N(6)-benzyladenosines, which are known to possess pronounced
Jinyun Dong et al.
Bioorganic & medicinal chemistry, 22(24), 6876-6884 (2014-12-04)
Bcr-Abl plays an essential role in the pathogenesis and development of chronic myeloid leukaemia (CML). Inhibition of Bcr-Abl has great potential for therapeutic intervention in CML. In order to obtain novel and potent Bcr-Abl inhibitors, twenty seven 4,6-disubstituted pyrimidines were
H Yockell-Lelièvre et al.
The Analyst, 140(15), 5105-5111 (2015-06-03)
The ability to detect small molecules in a rapid and sensitive manner is of great importance in the field of clinical chemistry, and the advancement of novel biosensors is key to realising point-of-care analysis for essential targets. Testosterone is an
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