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1.
Beech CL Coope JF Fairley G Gilbert PS Main BG Plé K 《The Journal of organic chemistry》2001,66(7):2240-2245
A new "safety catch" linker for esters has been synthesized on polystyrene resin. This 2-tert-butoxyphenol resin 10 may be acylated to give a relatively stable ester that will allow nucleophilic chemistry without reaction at the linking ester group. Removal of the tert-butyl group with acid unmasks a highly reactive 2-hydroxyphenyl ester that reacts readily with nucleophiles to cause release of the product from the resin. This sequence has been exemplified by acylating the resin with various bromo acids, carrying out nucleophilic displacements with thiols, phenols, or amines, activating the ester with trifluoroacetic acid and cleaving from the resin with amines to give the (nucleophile) substituted carboxamides in high yield and purity. Kinetic studies with a model ester revealed half-lives for reaction with morpholine of 119 h for the tert-butoxyphenyl ester and 1 min for the corresponding phenol. 相似文献
2.
M. Sc. Yasemin Akbulut Hannah J. Gaunt Prof. Katsuhiko Muraki Dr. Melanie J. Ludlow Dr. Mohamed S. Amer Dr. Alexander Bruns Dr. Naveen S. Vasudev Dr. Lea Radtke Dr. Matthieu Willot M. Sc. Sven Hahn M. Sc. Tobias Seitz Dr. Slava Ziegler Prof. Dr. Mathias Christmann Prof. Dr. David J. Beech Prof. Dr. Herbert Waldmann 《Angewandte Chemie (International ed. in English)》2015,54(12):3787-3791
Current therapies for common types of cancer such as renal cell cancer are often ineffective and unspecific, and novel pharmacological targets and approaches are in high demand. Here we show the unexpected possibility for the rapid and selective killing of renal cancer cells through activation of calcium‐permeable nonselective transient receptor potential canonical (TRPC) calcium channels by the sesquiterpene (?)‐englerin A. This compound was found to be a highly efficient, fast‐acting, potent, selective, and direct stimulator of TRPC4 and TRPC5 channels. TRPC4/5 activation through a high‐affinity extracellular (?)‐englerin A binding site may open up novel opportunities for drug discovery aimed at renal cancer. 相似文献
3.
Cumulant functions are introduced to describe the statistical state of a radiation field. These functions are simply related
to the optical coherence functions but have some interesting features. It is shown that if the cumulant functions of all orders
greater than some numberN
0 vanish then they also vanish for all orders greater than 2. Thermal field is the only field having this property. This property
holds whether the field is described by a classical stochastic process or by a quantum density operator. Further the particular
operator ordering used in defining these cumulant functions for the quantized field affects only the second order cumulant
function. To describe the statistical state of a vector field such as partially polarized or unpolarized radiation, one would
need to introduce cumulant tensors. 相似文献
4.
D. R. Beech C. Booth D. V. Dodgson I. H. Hillier 《Journal of Polymer Science.Polymer Physics》1972,10(8):1555-1564
The crystallization kinetics of a range of fractions of poly(ethylene oxide) are presented and analyzed. It is concluded that deviations from the Avrami equation with exponent of 3 are mainly due to rejection of low molecular weight molecules for the low molecular weight fractions (M?n < 6,000) and to a process of crystal perfecting for the high molecular weight fractions (M?n > 6,000). 相似文献
5.
We present the use of a simple microfluidic technique to separate living parasites from human blood. Parasitic trypanosomatids cause a range of human and animal diseases. African trypanosomes, responsible for human African trypanosomiasis (sleeping sickness), live free in the blood and other tissue fluids. Diagnosis relies on detection and due to their often low numbers against an overwhelming background of predominantly red blood cells it is crucial to separate the parasites from the blood. By modifying the method of deterministic lateral displacement, confining parasites and red blood cells in channels of optimized depth which accentuates morphological differences, we were able to achieve separation thus offering a potential route to diagnostics. 相似文献
6.
A Mejia R Shirazi R Beech D Balmer 《The Journal of the Operational Research Society》1998,49(1):33-41
This paper describes a simulation model of maternity services which was developed to support the planning of midwifery services to meet demands for continuity of care. A Government report of maternity services in 1992 emphasised the need to replace the fragmented care offered to pregnant women by a more personalised type of approach. One way of doing this is by the implementation of team midwifery in which care is provided, antenatally, during labour, and then postnatally by either the same midwife or, more usually a small team of midwives.The model described in this paper attempts to assess the effects of team size upon the continuity of care provided to pregnant women under different implementations. Continuity is measured in terms of the percentage of occasions a team midwife will be available to meet the health care demands of pregnant women. The model may be used not only for the evaluation of services already in use, but also for the planning of alternative and better services. 相似文献
7.
MA Freitas CL Hendrickson AG Marshall 《Rapid communications in mass spectrometry : RCM》1999,13(15):1639-1642
We present a novel approach for the determination of activation energy for the unimolecular dissociation of a large (>50 atoms) ion, based on measurement of the unimolecular dissociation rate constant as a function of continuous-wave CO(2) laser intensity. Following a short ( approximately 1 s) induction period, CO(2) laser irradiation produces an essentially blackbody internal energy distribution, whose 'temperature' varies inversely with laser intensity. The only currently available method for measuring such activation energies is blackbody infrared radiative dissociation (BIRD). Compared with BIRD, FRAGMENT: (a) eliminates the need to heat the surrounding ion trap and vacuum chamber to each of several temperatures (each requiring hours for temperature equilibration); (b) offers a three-fold wider range of effective blackbody temperature; and (c) extends the range of applications to include initially cold ions (e.g., gas-phase H/D exchange). Our FRAGMENT-determined activation energy for dissociation of protonated bradykinin, 1.2 +/- 0.1 eV, agrees within experimental error to the value, 1.3 +/- 0.1 eV, previously reported by Williams et al. from BIRD experiments. Copyright 1999 John Wiley & Sons, Ltd. 相似文献
8.
Arce FT Avci R Beech IB Cooksey KE Wigglesworth-Cooksey B 《Langmuir : the ACS journal of surfaces and colloids》2006,22(17):7217-7225
Atomic force microscopy (AFM) was combined with surface analytical techniques to investigate the rarely addressed issue of the effect of seawater on the surface properties of a selected fouling-release coating, silicon elastomer RTV11 (trademark of General Electric). The exposure of the RTV11 surface to seawater resulted in a modification of its morphology and mechanical properties, as confirmed by AFM and scanning electron microscopy (SEM). Surface modification was dependent on sample preparation and curing process, namely, curing agent concentration and relative humidity during curing. The RTV11 surface remained largely unaltered for samples cured under 100% relative humidity. SEM and X-ray photoelectron spectroscopy studies confirmed that the modified surface of RTV11 had the same elemental composition as the unexposed surface of the elastomer and showed excess Ca. However, the modified surface deformed plastically under load and was stiffer than the original surface. No major change was found on surfaces exposed to nanopure water during similar times of exposure as in seawater, regardless of curing conditions. The rate of increase in the aggregate formation in seawater can be described by an exponential function, with a decay constant of approximately 4.99 x 10(-)(3) min(-)(1) and a pre-exponential factor of approximately 1.77 x 10(-)(2) microm/min. 相似文献
9.
A number of physical techniques including scanning calorimetry and electron paramagnetic resonance have been used in an attempt to elucidate the course of the decomposition reaction of pyridine perchromate. 相似文献
10.
We describe how the elastomeric properties of PDMS (polydimethylsiloxane) can be utilised to achieve tuneable particle separation in Deterministic Lateral Displacement devices via strain controlled alteration of inter-obstacle distances, a development that opens up new avenues toward more effective separation of particles in microfluidics devices. 相似文献