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Showing 1-30 of 293 results for "59356-U" within Papers
Jin Zhang et al.
Nature, 509(7498), 119-122 (2014-05-03)
The P2Y12 receptor (P2Y12R), one of eight members of the P2YR family expressed in humans, is one of the most prominent clinical drug targets for inhibition of platelet aggregation. Although mutagenesis and modelling studies of the P2Y12R provided useful insights
Dongyin Chen et al.
Organic & biomolecular chemistry, 14(47), 11154-11161 (2016-11-11)
A one-pot highly specific isomerization of oleanolic acid esters (5a-g) to δ-oleanolic acid esters (6a-g) was achieved in the presence of proton-exchanged montmorillonite (H-mont) under mild reaction conditions. This protocol could proceed smoothly on a 15.0 gram scale. Based on
Eddie Chan et al.
Biochimica et biophysica acta, 1863(4), 638-649 (2016-01-18)
Cell migration is dependent on the microtubule network for structural support as well as for the proper delivery and positioning of polarity proteins at the leading edge of migrating cells. Identification of drugs that target cytoskeletal-dependent cell migration and protein
Atsushi Fukunari et al.
The Journal of pharmacology and experimental therapeutics, 311(2), 519-528 (2004-06-11)
Y-700 (1-[3-Cyano-4-(2,2-dimethylpropoxy)phenyl]-1H-pyrazole-4-carboxylic acid) is a newly synthesized inhibitor of xanthine oxidoreductase (XOR). Steady-state kinetics with the bovine milk enzyme indicated a mixed type inhibition with K(i) and K(i) ' values of 0.6 and 3.2 nM, respectively. Titration experiments showed that
Brian J Arey et al.
Endocrinology, 146(4), 2015-2022 (2005-01-08)
Circulating calcium (Ca(2+)) is a primary regulator of bone homeostasis through its action on PTH secretion. Extracellular Ca(2+) modulates PTH secretion through a cell surface G protein-coupled receptor, the calcium-sensing receptor (CaR). The expression of the CaR suggests a critical
Le Wang et al.
Journal of medicinal chemistry, 47(3), 612-626 (2004-01-23)
A novel series of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles have been synthesized as selective farnesyltransferase inhibitors using structure-based design. X-ray cocrystal structures of compound 20-FTase-HFP and A313326-FTase-HFP confirmed our initial design. The decreased interaction between the aryl groups and Ser 48 in GGTase-I binding
Lawrence F Colwell et al.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, 772(1), 89-98 (2002-05-23)
A generic isocratic HPLC-APCI-MS-MS method has been developed for the determination of plasma concentrations of bioactive compounds for the selection of potential new drug discovery candidates. A 4.6 x 50 mm cyano phase column eluted with an acetonitrile/water mobile phase
Maris A Cinelli et al.
Journal of medicinal chemistry, 60(9), 3958-3978 (2017-04-20)
Neuronal nitric oxide synthase (nNOS) inhibition is a promising strategy to treat neurodegenerative disorders, but the development of nNOS inhibitors is often hindered by poor pharmacokinetics. We previously developed a class of membrane-permeable 2-aminoquinoline inhibitors and later rearranged the scaffold
Arnout Voet et al.
ChemMedChem, 8(4), 644-651 (2013-02-26)
Unraveling the mechanisms involved in castration- and therapy-resistant prostate cancer has led to a renewed interest in androgen receptor (AR)-targeted therapeutics. Anti-androgens that block the activity of the AR therefore remain a valid therapeutic option. However, they must be more
Angelica Linton et al.
Journal of medicinal chemistry, 54(21), 7705-7712 (2011-10-01)
N-{trans-3-[(5-Cyano-6-methylpyridin-2-yl)oxy]-2,2,4,4-tetramethylcyclobutyl}imidazo[1,2-a]pyrimidine-3-carboxamide (1) was recently identified as a full antagonist of the androgen receptor, demonstrating excellent in vivo tumor growth inhibition in castration-resistant prostate cancer (CRPC). However, the imidazo[1,2-a]pyrimidine moiety is rapidly metabolized by aldehyde oxidase (AO). The present paper describes
Kerry A Ness et al.
Bioorganic & medicinal chemistry letters, 25(23), 5642-5645 (2015-11-03)
This Letter describes the continued SAR exploration of small molecule Legumain inhibitors with the aim of developing a potent and selective in vitro tool compound. Work continued in this Letter explores the use of alternative P2-P3 linker units and the
A Odawara et al.
Biochemical and biophysical research communications, 443(4), 1176-1181 (2014-01-11)
Human induced pluripotent stem cell (hiPSC)-derived neurons may be effectively used for drug discovery and cell-based therapy. However, the immaturity of cultured human iPSC-derived neurons and the lack of established functional evaluation methods are problematic. We here used a multi-electrode
Jesus R Medina et al.
The Journal of organic chemistry, 73(10), 3946-3949 (2008-04-24)
The synthesis of racemic nitrile (+/-)-9 was accomplished in four steps and 58% overall yield from the known pyrrolidinone 5. Nitrile (+/-)-9 was resolved via preparative chiral HPLC to afford optically pure nitriles (+)-9 and (-)-9, from which 3,3-dimethylprolines (+)-1
Roberto Pellicciari et al.
Journal of medicinal chemistry, 61(3), 745-759 (2018-01-19)
NAD
Sébastien Lethu et al.
Journal of medicinal chemistry, 52(20), 6205-6208 (2009-09-24)
Screening of the ICSN chemical library led to the discovery of 3-(4-chlorophenyl)-4-cyano-5-thioalkylthiophene 2-carboxylic acids as potent farnesyltransferase inhibitors. Enzymatic kinetic studies showed that this original FTI series belongs to the CaaX competitive inhibitor class. Preliminary SAR studies allowed us to
Bo Wang et al.
Pharmacological research, 122, 66-77 (2017-06-03)
Histone lysine specific demethylase 1 (LSD1) plays an important role in epigenetic modifications, and aberrant expression of LSD1 predicts tumor progression and poor prognosis in human esophageal cancers. In this study, a series of LSD1 inhibitors were synthesized and proved
Parul Mehrotra et al.
Bio Systems, 155, 1-9 (2017-03-07)
Modulation of host metabolic machinery by Mycobacterium tuberculosis is a well established phenomenon. In our earlier study (Mehrotra et al., 2014), we observed a marked increase in acetyl-CoA levels in cells bearing virulent M. tuberculosis infections compared to host cells
S Ishibuchi et al.
Bioorganic & medicinal chemistry letters, 11(7), 879-882 (2001-04-11)
A series of 1-phenylpyrazoles was evaluated for inhibitory activity against xanthine oxidase in vitro. Of the compounds prepared, 1-(3-cyano-4-neopentyloxyphenyl)pyrazole-4-carboxylic acid (Y-700) had the most potent enzyme inhibition and displayed longer-lasting hypouricemic action than did allopurinol in a rat model of
Angelica M Bello et al.
Journal of medicinal chemistry, 51(3), 439-448 (2008-01-15)
Malaria, caused by Plasmodia parasites, has re-emerged as a major problem, imposing its fatal effects on human health, especially due to multidrug resistance. In Plasmodia, orotidine 5'-monophosphate decarboxylase (ODCase) is an essential enzyme for the de novo synthesis of uridine
Naoki Kaneko et al.
Leukemia research, 37(9), 1156-1161 (2013-06-12)
Survivin and STAT3 pathway have been reported to be important for the growth of diffuse large B-cell lymphoma (DLBCL) cells. Here we investigated the antitumor activity of sepantronium bromide (YM155), a survivin suppressant, in combination with STAT3 inhibitors in DLBCL
Suqing Zheng et al.
Journal of labelled compounds & radiopharmaceuticals, 57(10), 606-610 (2014-09-10)
Tricyclic bis(cyanoenone), TBE-31, one of the most potent activators of the Keap1/Nrf2/antioxidant response element pathway, has been developed as a new anti-inflammatory and cytoprotective agent. (13) C2 (15) N2 -labeled TBE-31 ([(13) C2 (15) N2 ]-TBE-31), which has two (13)
Daniel M Walden et al.
Accounts of chemical research, 49(6), 1279-1291 (2016-06-09)
The flexibility, complexity, and size of contemporary organocatalytic transformations pose interesting and powerful opportunities to computational and experimental chemists alike. In this Account, we disclose our recent computational investigations of three branches of organocatalysis in which nonbonding interactions, such as
Graciela B Arhancet et al.
Journal of medicinal chemistry, 53(16), 5970-5978 (2010-08-03)
A new 1,4-dihydropyridine 5a, containing a cyano group at the C3 position, was recently reported to possess excellent mineralocorticoid receptor (MR) antagonist in vitro potency and no calcium channel-blocker (CCB) activity. In the present study, we report the structure-activity relationships
W C Rose et al.
Cancer research, 61(20), 7507-7517 (2001-10-19)
BMS-214662 is a potent and selective inhibitor of farnesyltransferase (FTI). In rodent fibroblasts transformed by oncogenes, BMS-214662 reversed the H-Ras-transformed phenotype but not that of K-Ras or other oncogenes. In soft agar growth assays, BMS-214662 showed good potency in inhibiting
Semin Lee et al.
Nature chemistry, 5(8), 704-710 (2013-07-25)
Since the discovery of crown ethers, macrocycles have been recognized as powerful platforms for supramolecular chemistry. Although their numbers and variations are now legion, macrocycles that are simple to make using high-yielding reactions in one pot and on the multigram
W Ho et al.
Journal of medicinal chemistry, 38(5), 794-802 (1995-03-03)
In previous papers, we have described the discovery of a new series of compounds, 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1 H)- ones, TlBO (1 and 1a), with potent anti-HIV-1 activity and the synthesis of analogues to better define the structure-activity relationships (SAR) in terms of
Songpo Guo et al.
Bioorganic & medicinal chemistry, 17(20), 7126-7130 (2009-09-29)
Indolo[2,3-a]carbazole based inhibitors were synthesized from readily available indigo via a seven-step linear synthetic sequence with a moderate overall yield. The inhibitors were selectively and readily functionalized at the nitrogen on the indole portion of the carbazole unit. The synthesized
P C Astles et al.
Journal of medicinal chemistry, 41(15), 2745-2753 (1998-07-21)
This publication describes the synthesis and optimization of a novel series of stilbene endothelin antagonists. Analysis of the SAR established for previous papers in this series prompted the design and synthesis of (Z)-4-phenyl-5-(3-benzyloxyphenyl)pent-4-enoic acid 3 which was found to be
S E Yoo et al.
Journal of medicinal chemistry, 44(24), 4207-4215 (2001-11-16)
This paper describes the design, synthesis, and biological evaluation of a novel anti-ischemic compound, (2S,3S,4R)-N-(6-amino-3,4-dihydro-2-dimethoxymethyl-3-hydroxy-2-methyl-2H-benzopyranyl)-N'-benzyl-N"-cyanoguanidine (33), and the structure-activity relationships leading to the discovery of this compound. Compound 33 significantly reduced the myocardial infarct zone to area at risk (IZ/AAR)
Tadashi Honda et al.
Bioorganic & medicinal chemistry letters, 21(8), 2188-2191 (2011-03-29)
To explore more potent N-acylimidazole analogues of CDDO than CDDO-Im, which is one of the most potent compounds in several widely used bioassays related to protection against inflammation and carcinogenesis; we have synthesized and evaluated five new N-acyl(acetylenic)imidazole analogues. Among
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