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Iodomethyl-, chloromethyl-, and fluoromethyldimethylsulfonium salts, 4b-d, have been synthesized and are observed to be highly reactive molecules that exhibit extraordinary diversity with respect to the nature of their reactivity, undergoing facile direct substitution (S(N)2) reactions, but also being highly susceptible to electron-transfer reactions. Cyclic voltametry experiments indicated that the iodomethyldimethylsulfonium compound, 4b, is a potent electron acceptor, even surpassing the reactivity of perfluoro-n-alkyl iodides in that capacity. The iodo- and chloromethyldimethylsulfonium salts, 4b,c, as well as the analogous iodomethyltrimethylammonium salt, 3a, are shown to be reactive SET acceptors. 相似文献
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Designer gene therapy using an Escherichia coli purine nucleoside phosphorylase/prodrug system 总被引:1,自引:0,他引:1
Bennett EM Anand R Allan PW Hassan AE Hong JS Levasseur DN McPherson DT Parker WB Secrist JA Sorscher EJ Townes TM Waud WR Ealick SE 《Chemistry & biology》2003,10(12):1173-1181
Activation of prodrugs by Escherichia coli purine nucleoside phosphorylase (PNP) provides a method for selectively killing tumor cells expressing a transfected PNP gene. This gene therapy approach requires matching a prodrug and a known enzymatic activity present only in tumor cells. The specificity of the method relies on avoiding prodrug cleavage by enzymes already present in the host cells or the intestinal flora. Using crystallographic and computer modeling methods as guides, we have redesigned E. coli PNP to cleave new prodrug substrates more efficiently than does the wild-type enzyme. In particular, the M64V PNP mutant cleaves 9-(6-deoxy-alpha-L-talofuranosyl)-6-methylpurine with a kcat/Km over 100 times greater than for native E. coli PNP. In a xenograft tumor experiment, this compound caused regression of tumors expressing the M64V PNP gene. 相似文献
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This laboratory exercise will expose upper-level undergraduate students to the aspect of chemistry known as Chemical Mechanical Planarization (CMP). CMP is used for the fabrication of computer chips and memory devices. Students investigate a representative slurry that is used for copper-based advanced integrated-circuit processes. More specifically, students monitor the generation of OH through the decomposition of hydrogen peroxide in the presence of a metal/amino acid complex, which is used as a catalyst. This introduces students to the fundamentals of OH trapping and provides practice in the techniques used for kinetic rate determination. The kinetics data obtained for these systems will be correlated with the static dissolution rate of Cu metal upon exposure to various control and hydroxyl radical generating solutions. 相似文献
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Brooks WH McCloskey DE Daniel KG Ealick SE Secrist JA Waud WR Pegg AE Guida WC 《Journal of chemical information and modeling》2007,47(5):1897-1905
In silico chemical library screening (virtual screening) was used to identify a novel lead compound capable of inhibiting S-adenosylmethionine decarboxylase (AdoMetDC). AdoMetDC is intimately involved in the biosynthesis of polyamines, which are essential for tumor progression and are elevated in numerous types of tumors. Therefore, inhibition of this enzyme provides an attractive target for the discovery of novel anticancer drugs. We performed virtual screening using a computer model derived from the X-ray crystal structure of human AdoMetDC and the National Cancer Institute's Diversity Set (1990 compounds). Our docking study suggested several compounds that could serve as drug candidates since their docking modes and scores revealed potential inhibitory activity toward AdoMetDC. Experimental testing of the top-scoring compounds indicated that one of these compounds (NSC 354961) possesses an IC50 in the low micromolar range. A search of the entire NCI compound collection for compounds similar to NSC 354961 yielded two additional compounds that exhibited activity in the experimental assay but with significantly diminished potency relative to NSC 354961. In this report, we disclose the activity of NSC 354961 against AdoMetDC and its probable binding mode based on computational modeling. We also discuss the importance of virtual screening in the context of enzymes that are not readily amenable to high-throughput assays, thereby demonstrating the efficacy of virtual screening, combined with selective experimental testing, in identifying new potential drug candidates. 相似文献
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A mathematical model describing the coupling of electrical,optical and thermal effects in semiconductor lasers is introduced.Numerical and asymptotic solutions are derived, including expressionsfor key physical quantities such as the initial time delay,the frequency of spike oscillation and the temperature rise,together with its influence on the photon density, the electronconcentration and the threshold current. The consequences ofthermal effects in reducing efficiency are thus quantified. 相似文献
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BłAŻEJ JAN WRÓBEL 《Proceedings Mathematical Sciences》2011,121(1):45-75
We examine weighted L
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boundedness of g-functions based on semigroups related to multi-dimensional Laguerre function expansions of Hermite type. A technique of vector-valued
Calderón–Zygmund operators is used. 相似文献
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