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Stefan Peterli Dieter Hubmann Urs Squin Helmut Mett Peter Traxler 《Helvetica chimica acta》1994,77(1):59-69
β-Nitrostyrene derivatives of adenosine 5′-glutarates are potent and selective bisubstrate-type inhibitors of the epidermal growth factor receptor protein tyrosine kinase (EGF-R PTK). In an attempt to improve the inhibitory activity, this type of compounds was modified with alkyl spacers of varying length between the nitrostyrene and the glutaryl units. The spacers consisted of 1, 3, 4, and 5 atoms to give compounds of the benzyl, oxyethyl, oxypropyl, and oxybutyl series, respectively (Schemes 1 and 2). Adenosine 5′-esters were prepared in the benzyl and oxypropyl series only. Compared to the compounds in the parent series without spacer (IC50 = 0.7–12 μM ), most of the modified compounds inhibited the EGF-R PTK only marginally or were inactive (IC50 ≥ 100 μM ). The only exceptions were the free acids 19 and 20 with IC50 values of ca. 5 μM . It is noteworthy that esterification of these two hydrogen glutarates with either MeOH or adenosine yielded inactive compounds, which is in contrast to the corresponding substances without spacers. 相似文献
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Helmut Schmidhammer Eva Scherb-Bukowiecki Thomas A. Mayer Peter Schnholzer 《Helvetica chimica acta》1994,77(6):1590-1594
The synthesis of benzazepine analogues of the opium alkaloid noscapine ( 1 ) is described. The benzazepines 2 and 3 were prepared starting from nornarceine ethyl ester ( 4 ; readily available from 1 ) in several steps. X-Ray analysis of compound 2 revealed that it is not a diastereosisomer mixture but a racemate of the threo-form and thus has the same configuration as 1 . 相似文献
6.
Michel Weber 《Transactions of the American Mathematical Society》2006,358(2):911-936
We apply a majorizing measure theorem of Talagrand to obtain uniform bounds for sums of random variables satisfying increment conditions of the type considered in Gál-Koksma Theorems. We give some applications.
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O. Kortner M.P. Locher V.E. Markushin P. Weber O. Wigger 《The European Physical Journal C - Particles and Fields》2002,25(3):353-360
We study correlations in the exclusive reaction at rest with complete reconstruction of the kinematics for each event. The inclusive distribution is fairly flat at small
invariant mass of the pion pair while a small enhancement in the double differential distribution is observed for small invariant
masses of both pion pairs. Dynamical models with resonances in the final state are shown to be consistent with the data while
the stochastic HBT mechanism is not supported by the present findings.
Received: 26 February 2002 / Revised version: 22 July 2002 / Published online: 30 August 2002 相似文献
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Michel Weber 《Results in Mathematics》2005,47(3-4):340-354
Under a very moderate assumption on the Fourier coefficients of a periodic function, we show the convergence almost everywhere of the sequence of averages of its associated Riemann sums. The structure of the set of averages is analyzed by proving a spectral regularization type inequality, which allows to control the corresponding Littlewood-Paley square function. 相似文献
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Kenneth Weber Vilmar Trevisan Luiz Felipe Martins 《Journal of Algorithms in Cognition, Informatics and Logic》2005,54(2):152-167
This paper describes the first algorithm to compute the greatest common divisor (GCD) of two n-bit integers using a modular representation for intermediate values U, V and also for the result. It is based on a reduction step, similar to one used in the accelerated algorithm [T. Jebelean, A generalization of the binary GCD algorithm, in: ISSAC '93: International Symposium on Symbolic and Algebraic Computation, Kiev, Ukraine, 1993, pp. 111–116; K. Weber, The accelerated integer GCD algorithm, ACM Trans. Math. Softw. 21 (1995) 111–122] when U and V are close to the same size, that replaces U by (U−bV)/p, where p is one of the prime moduli and b is the unique integer in the interval (−p/2,p/2) such that . When the algorithm is executed on a bit common CRCW PRAM with O(nlognlogloglogn) processors, it takes O(n) time in the worst case. A heuristic model of the average case yields O(n/logn) time on the same number of processors. 相似文献
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