- Grafting Behavior for the Resonating Variants of Ethynylaniline on Hydrogenated Silicon (100) Surfaces under Thermal Hydrosilylation
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This work reports the outcome of thermal grafting of 2-ethynylaniline, 3-ethynylaniline, and 4-ethynylaniline on a hydrogenated Si(100) surface. Using high-resolution XPS and AFM, it was found that the grafting of these compounds could be attributed to re
- Tung, Joline,Tew, Lih Shin,Coluccini, Carmine,Lin, Yue-Der,Khung, Yit Lung
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Read Online
- Fragment screening and assembly: A highly efficient approach to a selective and cell active protein tyrosine phosphatase 1B inhibitor
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Using an NMR-based fragment screening and X-ray crystal structure-based assembly, starting with millimolar ligands for both the catalytic site and the second phosphotyrosine binding site, we have identified a small-molecule inhibitor of protein tyrosine phosphatase 1B with low micromolar inhibition constant, high selectivity (30-fold) over the highly homologous T-cell protein tyrosine phosphatase, and good cellular activity in COS-7 cells.
- Liu, Gang,Xin, Zhili,Pei, Zhonghua,Hajduk, Philip J.,Abad-Zapatero, Cele,Hutchins, Charles W.,Zhao, Hongyu,Lubben, Thomas H.,Ballaron, Stephen J.,Haasch, Deanna L.,Kaszubska, Wiweka,Rondinone, Cristina M.,Trevillyan, James M.,Jirousek, Michael R.
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Read Online
- A relay FRET event in a designed trichromophoric pentapeptide containing an: O -, m -aromatic-amino acid scaffold
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The concept of a relay FRET event is established in a designed trichromophoric pentapeptide containing an o-,m-aromatic amino acid scaffold in the backbone as a novel β-turn mimetic β-sheet folding nucleator. This system would find application in studying fundamental processes involving interbiomolecular interactions in chemical biology.
- Bag, Subhendu Sekhar,Yashmeen, Afsana
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Read Online
- GLUCOCORTICOID RECEPTOR AGONIST AND IMMUNOCONJUGATES THEREOF
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Provided herein are glucocorticoid receptor agonist immunoconjugates, glucocorticoid receptor agonists, and methods of using the same, e.g., to treat autoimmune or inflammatory diseases.
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Paragraph 001146; 001147
(2018/01/17)
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- Axially chiral amino acid scaffolds as efficient fluorescent discriminators of methanol-ethanol
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We report a unique fluorescence sensor based on an axially chiral unnatural triazolyl aromatic amino acid scaffold (ArTAA) for discrimination of methanol from ethanol via a switch on fluorescence response. All three sensors, the simple scaffold (ArTAA), and the mono- (PyAm-ArTAA) and bis-pyrenyl- (Py2Am-ArTAA) amides, show similar sensitivity and detection limit ranging from 0.5-2.1 v/v% of ethanol. The solid films of these sensors are also found to be effective in sensing ethanol vapour via generation of a distinct and enhanced fluorescence signal. All our experimental results suggest the role of axial chirality of the hairpin-shaped scaffold in differential solvation guided H-bonding interaction and discriminating between ethanol and methanol with a switch-on fluorescence response.
- Bag, Subhendu Sekhar,Jana, Subhashis
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supporting information
p. 13391 - 13398
(2017/11/28)
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- Cu-Catalyzed Aminodifluoroalkylation of Alkynes and α-Bromodifluoroacetamides
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The copper-catalyzed highly regioselective aminodifluoroalkylation of alkynes and α-bromodifluoroacetamides was realized for the first time. With this method, 3,3-difluoro-1H-pyrrol-2(3H)-ones were constructed in a single step from various alkynes and α-b
- Lv, Yunhe,Pu, Weiya,Chen, Qian,Wang, Qingqing,Niu, Jiejie,Zhang, Qian
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p. 8282 - 8289
(2017/08/14)
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- Triazolo-β-aza-ε-amino acid and its aromatic analogue as novel scaffolds for β-turn peptidomimetics
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Triazolo-β-aza-ε-amino acid and its aromatic analogue (AlTAA/ArTAA) in the peptide backbone mark a novel class of conformationally constrained molecular scaffolds to induce β-turn conformations. This was demonstrated forAlTAA in a Leu-enkephalin analogue and in a designed pentapeptide wherein the FRET process was established. Restricted rotation induced chirality and turn conformation into the achiral aromatic amino acid scaffold,ArTAA, which in a short tripeptide backbone acted as a β-turn mimic as a β-sheet folding nucleator. This journal is
- Bag, Subhendu Sekhar,Jana, Subhashis,Yashmeen, Afsana,De, Suranjan
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supporting information
p. 5242 - 5245
(2015/03/30)
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- Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. A potent and selective series for further drug development
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New antituberculosis (anti-TB) drugs are urgently needed to shorten the 6-12month treatment regimen and especially to battle drug-resistant Mycobacterium tuberculosis (Mtb) strains. In this study, we have continued our efforts to develop isoxazole-based a
- Lilienkampf, Annamaria,Pieroni, Marco,Wan, Baojie,Wang, Yuehong,Franzblau, Scott G.,Kozikowski, Alan P.
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scheme or table
p. 678 - 688
(2010/07/06)
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- AMINO-5-[4-(DIFLUOROMETHOXY)PHENYL]-5-PHENYLIMIDAZOLONE COMPOUNDS FOR THE INHIBITION OF BETA-SECRETASE
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The present invention provides compounds and methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
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Page/Page column 39-40
(2009/03/07)
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- SULFOXIMINES AS KINASE INHIBITORS
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The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
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Page/Page column 71
(2008/12/05)
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- Use of the Nitrile Oxide Cycloaddition (NOC) reaction for molecular probe generation: A new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6
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A series of hydroxamate based HDAC inhibitors containing a phenylisoxazole as the CAP group has been synthesized using nitrile oxide cycloaddition chemistry. An HDAC6 selective inhibitor having a potency of ~2 picomolar was identified. Some of the compounds were examined for their ability to block pancreatic cancer cell growth and found to be about 10-fold more potent than SAHA. This research provides valuable, new molecular probes for use in exploring HDAC biology.
- Kozikowski, Alan P.,Tapadar, Subhasish,Luchini, Doris N.,Ki, Hwan Kim,Billadeau, Daniel D.
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supporting information; experimental part
p. 4370 - 4373
(2009/05/30)
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- PYRIMIDINES WITH TIE2 (TEK) ACTIVITY
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The invention relates to a compound of the Formula (I). or salt thereof wherein R1, R2, R3, R4, R5, R6, A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm-blooded animal. The invention also relates to processes for the preparation of said compounds.
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Page/Page column 148
(2010/02/12)
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- Protein-tyrosine phosphatase inhibitors and uses thereof
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The present invention is directed to compounds of formula (I), or a pharmaceutically suitable salt or prodrug thereof, which are useful for the selective inhibition of protein tyrosine phosphatase-1B (PTP1B), and are useful for the treatment of disorders caused by overexpressed or altered protein tyrosine phosphatase 1B.
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- Unsaturated amides derived from 2-amino-3-hydroxycyclopentenone: A Stille approach to the synthesis of asuka-mABA, 2880-II, and limocrocin
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A Stille palladium catalysed vinyl halide-vinyl stannane or aryl stannane coupling approach to the title compounds is described. The 2- aminocyclopentanedione-derived vinyl bromides (12, n = 1, 2, 3) were prepared and coupled to synthesise 2880-II (4), a Streptomyces metabolite, asuka-mABA (6), obtained during investigations to elucidate the biogenesis of the antibiotic asukamycin, and limocrocin (10), a naturally occurring antibiotic and antiviral agent.
- Macdonald, Gregor,Alcaraz, Lilian,Wei, Xudong,Lewis, Norman J.,Taylor, Richard J. K.
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p. 9823 - 9836
(2007/10/03)
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- A Stille approach to unsaturated amides derived from 2-amino-3-hydroxycyclopentenone: The synthesis of asuka-mABA and limocrocin
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A Stille palladium-catalysed vinyl halide-vinyl stannane coupling approach to the title compounds is described.
- Macdonald, Gregor,Lewis, Norman J.,Taylor, Richard J. K.
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p. 2647 - 2648
(2007/10/03)
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