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1.
Wender PA Baryza JL Bennett CE Bi FC Brenner SE Clarke MO Horan JC Kan C Lacôte E Lippa B Nell PG Turner TM 《Journal of the American Chemical Society》2002,124(46):13648-13649
Macrocycle 1 is a new highly potent analogue of bryostatin 1, a promising anti-cancer agent currently in human clinical trials. In vitro, 1 displays picomolar affinity for PKC and exhibits over 100-fold greater potency than bryostatin 1 when tested against various human cancer cell lines. Macrocycle 1 can be generated in clinically required amounts by chemical synthesis in only 19 steps (LLS) and represents a new clinical lead for the treatment of cancer. 相似文献
2.
Debora Vilona Prof. Moreno Lelli Prof. Elise Dumont Dr. Emmanuel Lacôte 《Chemistry (Weinheim an der Bergstrasse, Germany)》2021,27(71):17761-17764
Several urea-inserted organo-polyoxometalates (POMs) derived from polyoxotungstovanadate [P2V3W15O61]9− were prepared. The insertion of the carbonyl into the polyoxometallic framework activates the urea toward Hydrogen-bond catalysis. This was shown on the Friedel-Crafts arylation of trans-β-nitrostyrene. Modelling shows that the most stable form of the organo-POMs features a cis-trans arrangement of the two N−H bonds, but that the likely catalytically active trans-trans form is accessible at room temperature. Finally, it is possible that the oxo substituents next to the vanadium atoms may help the approach of the nucleophile via H-bonding. 相似文献
3.
Specific ion effects on the electrophoretic mobility of small,highly charged peptides: A modeling study
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Stuart A. Allison Hengfu Wu Tuyen M. Bui Lac Dang Giang H. Huynh Tam Nguyen Linda Soegiarto Bi C. Truong 《Journal of separation science》2014,37(17):2403-2410
In this work, we use coarse‐grained modeling to study the free solution electrophoretic mobility of small highly charged peptides (lysine, arginine, and short oligos thereof (up to nonapeptides)) in NaCl and Na2SO4 aqueous solutions at neutral pH and room temperature. The experimental data are taken from the literature. A bead modeling methodology that treats the electrostatics at the level of the nonlinear Poisson Boltzmann equation developed previously in our laboratory is able to account for the mobility of all peptides in NaCl, but not Na2SO4. The peptide mobilities in Na2SO4 can be accounted for by including sulfate binding in the model and this is proposed as one possible explanation for the discrepancy. Oligo arginine peptides bind more sulfate than oligo lysines and sulfate binding increases with the oligo length. 相似文献
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Igor Krupa Tomáš Nedelčev Dušan Račko Igor Lacík 《Journal of Sol-Gel Science and Technology》2010,53(1):107-114
The mechanical properties for silica hydrogel prepared at physiological conditions are reported in this paper. The mechanical
testing was performed in the compression mode determining the mechanical characteristics as a function of aging time in TRIS
buffer up to 14 days. In addition to a typically used gradient method for Young’s modulus determination from the stress–strain
curves, a new phenomenological model was proposed to describe the experimental data. The mechanical properties were stabilized
after 2 days of aging, which was concluded from an increase in Young’s modulus between 90 and 400 kPa, an increase in stress
at break between 50 and 100 kPa and by a decrease in relative deformation at break from 0.26 to 0.16. The height of samples
was constant in the first three days of aging followed by a decrease by ~20%. Dissolving of silica hydrogel characterized
through determination of silica content in TRIS buffer employing the molybdenum method was not found to be responsible for
this phenomenon. The phenomenological model is proposed to be used for a reliable evaluation of mechanical properties of silica
as well as other hydrogels exhibiting low Young’s modulus. 相似文献
7.
Nathalie Dupré Pauline Rémy Dr. Kévin Micoine Dr. Cécile Boglio Dr. Serge Thorimbert Dr. Emmanuel Lacôte Dr. Bernold Hasenknopf Prof. Max Malacria Prof. 《Chemistry (Weinheim an der Bergstrasse, Germany)》2010,16(24):7256-7264
The preparation of new organosoluble Lewis acidic polyoxometalates (POMs) is reported. These complexes were prepared by the incorporation of Zr, Sc, and Y atoms into the corresponding monolacunary Dawson [P2W17O61]10? and Keggin [PW11O39]7? polyoxotungstates. The catalytic activity of these compounds was evaluated for C? C bond formation in the Diels–Alder, Mannich, and Mukaiyama‐type reactions. Comparisons with previously described Lewis acidic POMs are reported. Competitive reactions between imines and aldehydes or between various imines demonstrated that fine tuning of the reactivity could be reached by varying the metal atom incorporated into the polyanionic framework. A series of experiments that employed pyridine derivatives allowed us to distinguish between the Lewis and induced Brønsted acidity of the POMs. These catalysts activate imines in a Lewis acidic way, whereas aldehydes are activated by indirect Brønsted catalysis. 相似文献
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N,N'-dialkyl and N,N'-diaryl imidazol-2-ylidene-boranes and trifluoroboranes are rapidly lithiated at C4 of the imidazole ring, and the resulting intermediates have been quenched with an assortment of electrophiles to provide ring-functionalized imidazol-2-ylidene-boranes. Further deprotonation and functionalization of C5 have been demonstrated. Deboronation of the products by treatment with triflic acid or iodine and then methanol opens a route to C4/C5 functionalized imidazolium salts and imidazol-2-ylidenes. 相似文献
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Strohhöfer C Förster T Chorvát D Kasák P Lacík I Koukaki M Karamanou S Economou A 《Physical chemistry chemical physics : PCCP》2011,13(39):17852-17863
This article reports the full characterisation of the optical properties of a biosynthesised protein consisting of fused cyan fluorescent protein, glucose binding protein and yellow fluorescent protein. The cyan and yellow fluorescent proteins act as donors and acceptors for intramolecular fluorescence resonance energy transfer. Absorption, fluorescence, excitation and fluorescence decays of the compound protein were measured and compared with those of free fluorescent proteins. Signatures of energy transfer were identified in the spectral intensities and fluorescence decays. A model describing the fluorescence properties including energy transfer in terms of rate equations is presented and all relevant parameters are extracted from the measurements. The compound protein changes conformation on binding with calcium ions. This is reflected in a change of energy transfer efficiency between the fluorescent proteins. We track the conformational change and the kinetics of the calcium binding reaction from fluorescence intensity and decay measurements and interpret the results in light of the rate equation model. This visualisation of change in protein conformation has the potential to serve as an analytical tool in the study of protein structure changes in real time, in the development of biosensor proteins and in characterizing protein-drug interactions. 相似文献
10.
J. Ball C. D. Lac F. Lehar A. de Lesquen L. van Rossum P. Chaumette J. Derégel J. Fabre M. de Mali J. M. Fontaine F. Perrot P. Bach G. Gaillard R. Hess D. Rapin Ph. Sormani V. Ghazikhanian C. A. Whitten R. Peschina E. Rössle 《Zeitschrift fur Physik C Particles and Fields》1988,40(2):193-197
We present the measurements of the spin correlation parameterA ookk (np). A longitudinally polarized beam of free neutrons obtained from the break-up of polarized deuterons was scattered on the longitudinally polarized Saclay frozen-spin proton target. Measurements were carried out at SATURNE II, at neutron beam kinetic energies of 0.63, 0.88, 0.98 and 1.08 GeV. The data points cover the angular region from about 40° to 110° CM. The observed angular dependence ofA ookk (np) at 0.63 GeV agree with the phase shift analysis predictions except at small angles. 相似文献