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1.
Fan Caiyun Jia Hongmei Deuther-Conrad Winnie Brust Peter Steinbach J?rg Liu Boli 《中国科学B辑(英文版)》2006,49(2):169-176
A novel 99mTc labeled complex, [N-[2-((2-oxo-2-(4-(3-phenylpropyl)piperazin-1-yl)ethyl) (2-mercaptoethyl)amino)acetyl]-2-aminoethanethiolato]Technetium(V)
oxide (PPPE-MAMA’-99mTcO) ([
99m
Tc]-2) has been designed and prepared based on the integrated approach. The corresponding rhenium complex (PPPE-MAMA’-ReO)(Re-2) has been prepared and characterized. In vitro competition binding assays show moderate affinity of Re-2 towards σ1 and σ2 receptors with K
i values of 8.67 ± 0.07 and 5.71 ± 1.88 μmol, respectively. Planar images obtained at 0.5 h, 4 h, 20 h after i.v. injection
indicate the accumulation of [
99m
Tc]-2 in MCF-7 human breast tumor bearing mice at 20 h. Furthermore, the accumulation of [
99m
Tc]-2 has been inhibited at 20 h after co-injection of [
99m
Tc]-2 plus haloperidol (1 mg/kg). Biodistribution studies of [
99m
Tc]-2 display an in vivo tumor uptake of 0.14% ± 0.01% ID/g at 24 h post i.v. injection with a tumor/muscle ratio of 6.02 ± 0.87. The above results
suggest that [
99m
Tc]-2, derived from a previously published lead compound, retains certain tumor uptake and affinity for σ receptors. [
99m
Tc]-2 may be used as a basis for further structural modifications to develop tumor imaging agents with high affinity for σ receptors. 相似文献
2.
Cyclodimerization versus Polymerization of Methyl Methacrylate Induced by N‐Heterocyclic Carbenes: A Combined Experimental and Theoretical Study
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Winnie Nzahou Ottou Damien Bourichon Dr. Joan Vignolle Anne‐Laure Wirotius Dr. Fredéric Robert Prof. Yannick Landais Dr. Jean‐Marc Sotiropoulos Dr. Karinne Miqueu Prof. Daniel Taton 《Chemistry (Weinheim an der Bergstrasse, Germany)》2014,20(14):3989-3997
The activation behavior of two N‐heterocyclic carbenes (NHCs), namely, 1,3‐bis(isopropyl)imidazol‐2‐ylidene(NHCiPr) and 1,3‐bis(tert‐butyl) imidazol‐2‐ylidene (NHCtBu), as organic nucleophiles in the reaction with methyl methacrylate (MMA) is described. NHCtBu allows the polymerization of MMA in DMF at room temperature and in toluene at 50 °C, whereas NHCiPr reacts with two molecules of MMA, forming an unprecedented imidazolium–enolate cyclodimer (NHCiPr/MMA=1:2). It is proposed that the reaction mechanism occurs by initial 1,4‐nucleophilic addition of NHCiPr to MMA, generating a zwitterionic enolate 2 , followed by addition of 2 to a second MMA molecule, forming a linear imidazolium–enolate 3 (NHCiPr/MMA=1:2). Proton transfer, generating intermediate 5 , followed by cyclization and release of methanol yielded the aforementioned zwitterionic cyclodimer 1:2 adduct 7 , the molecular structure of which has been established by NMR spectroscopy, X‐ray diffraction, and mass spectrometry. This unexpected difference between NHCtBu and NHCiPr in the reaction with MMA (polymerization and cyclodimerization, respectively) can be rationalized by using DFT calculations. In particular, the nature of the NHC strongly influences the cyclodimerization pathway, the cyclization of 5 and the release of methanol are the discriminating step and limiting step, respectively. In the case of NHCtBu, both steps are strongly disfavoured compared with that of NHCiPr (energetic difference of around 14 and 9 kcal mol?1, respectively), preventing the cyclization mechanism from a kinetic viewpoint. Moreover, addition of a third molecule of MMA in the polymerization pathway results in a lower activation barrier than that of the limiting step in the cyclodimerization pathway (difference of around 14 kcal mol?1), in agreement with the formation of polymethyl methacrylate (PMMA) by using NHCtBu as nucleophile. 相似文献
3.
From the N‐Heterocyclic Carbene‐Catalyzed Conjugate Addition of Alcohols to the Controlled Polymerization of (Meth)acrylates
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Winnie Nzahou Ottou Damien Bourichon Dr. Joan Vignolle Anne‐Laure Wirotius Dr. Fredéric Robert Prof. Yannick Landais Dr. Jean‐Marc Sotiropoulos Dr. Karinne Miqueu Prof. Daniel Taton 《Chemistry (Weinheim an der Bergstrasse, Germany)》2015,21(26):9447-9453
Among various N‐heterocyclic carbenes (NHCs) tested, only 1,3‐bis(tert‐butyl)imidazol‐2‐ylidene (NHCtBu) proved to selectively promote the catalytic conjugate addition of alcohols onto (meth)acrylate substrates. This rather rare example of NHC‐catalyzed 1,4‐addition of alcohols was investigated as a simple means to trigger the polymerization of both methyl methacrylate and methyl acrylate (MMA and MA, respectively). Well‐defined α‐alkoxy poly(methyl (meth)acrylate) (PM(M)A) chains, the molar masses of which could be controlled by the initial [(meth)acrylate]0/[ROH]0 molar ratio, were ultimately obtained in N,N‐dimethylformamide at 25 °C. A hydroxyl‐terminated poly(ethylene oxide) (PEO‐OH) macro‐initiator was also employed to directly access PEO‐b‐PMMA amphiphilic block copolymers. Investigations into the reaction mechanism by DFT calculations revealed the occurrence of two competitive concerted pathways, involving either the activation of the alcohol or that of the monomer by NHCtBu. 相似文献
4.
5.
Ming-Hsuan Kang Wen-Ching Winnie Li Chian-Jen Wang 《Israel Journal of Mathematics》2018,228(1):79-117
In this paper, we study relations between Langlands L-functions and zeta functions of geodesic walks and galleries for finite quotients of the apartments of G =PGL3 and PGSp4 over a nonarchimedean local field with q elements in its residue field. They give rise to an identity (Theorem 5.3) which can be regarded as a generalization of Ihara’s theorem for finite quotients of the Bruhat–Tits trees. This identity is shown to agree with the q = 1 version of the analogous identities for finite quotients of the building of G established in [KL14, KLW10, FLW13], verifying the philosophy of the field with one element by Tits. A new identity for finite quotients of the building of PGSp4 involving the standard L-function (Theorem 6.3), complementing the one in [FLW13] which involves the spin L-function, is also obtained. 相似文献
6.
Northen TR Woo HK Northen MT Nordström A Uritboonthail W Turner KL Siuzdak G 《Journal of the American Society for Mass Spectrometry》2007,18(11):1945-1949
The surface structure of porous silicon used in desorption/ionization on porous silicon (DIOS) mass analysis is known to play a primary role in the desorption/ionization (D/I) process. In this study, mass spectrometry and scanning electron microscopy (SEM) are used to examine the correlation between intact ion generation with surface ablation and surface morphology. The DIOS process is found to be highly laser energy dependent and correlates directly with the appearance of surface ions (Si(n)(+) and OSiH(+)). A threshold laser energy for DIOS is observed (10 mJ/cm(2)), which supports that DIOS is driven by surface restructuring and is not a strictly thermal process. In addition, three DIOS regimes are observed that correspond to surface restructuring and melting. These results suggest that higher surface area silicon substrates may enhance DIOS performance. A recent example that fits into this mechanism is the surface of silicon nanowires, which has a high surface energy and concomitantly requires lower laser energy for analyte desorption. 相似文献
7.
Li J Li WZ Huang W Cheung AW Bi CW Duan R Guo AJ Dong TT Tsim KW 《Journal of chromatography. A》2009,1216(11):2071-2078
A high-performance liquid chromatography coupled with diode array detector and mass spectrometry (HPLC-DAD-MS) method was developed to evaluate the quality of Rhizoma Belamcandae (Belamcanda chinensis (L.) DC.) through establishing chromatographic fingerprint and simultaneous determination of seven phenolic compounds. The analysis was achieved on an Alltima C(18) analytical column (250 mm x 4.6 mm i.d. 5 microm) using linear gradient elution of acetonitrile-0.1% trifluoroacetic acid. The correlation coefficients of similarity were determined from the HPLC fingerprints, and they shared a close similarity. By using an online APCI-MS/MS, twenty phenols were identified. In addition, seven of these phenols including mangiferin, 7-O-methylmangiferin, tectoridin, resveratrol, tectorigenin, irigenin and irisflorentin were quantified by the validated HPLC-DAD method. These phenols are considered to be major constituents in Rhizoma Belamcandae, and are generally regarded as the index for quality assessment of this herb. This developed method by having a combination of chromatographic fingerprint and quantification analysis could be applied to the quality control of Rhizoma Belamcandae. 相似文献
8.
Andrew Martin Winnie Kiarie Boyce Chang Martin Thuo 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2020,132(1):360-365
Studies on passivating oxides on liquid metals are challenging, in part, due to plasticity, entropic, and technological limitations. In alloys, compositional complexity in the passivating oxide(s) and underlying metal interface exacerbates these challenges. This nanoscale complexity, however, offers an opportunity to engineer the surface of the liquid metal under felicitous choice of processing conditions. We inferred that difference in reactivity, coupled with inherent interface ordering, presages exploitable order and selectivity to autonomously present compositionally biased oxides on the surface of these metals. Besides compositional differences, sequential release of biased (enriched) components, via fractal-like paths, allows for patterned layered surface structures. We, therefore, present a simple thermal-oxidative compositional inversion (TOCI) method to introduce fractal-like structures on the surface of these metals in a controlled (tier, composition, and structure) manner by exploiting underlying stochastic fracturing process. Using a ternary alloy, a three-tiered (in structure and composition) surface structure is demonstrated. 相似文献
9.
Valrie Weber Lucie Arnaud Sladjana Dukic-Stefanovic Barbara Wenzel Valrie Roux Jean-Michel Chezal Thu-Hang Lai Rodrigo Teodoro Klaus Kopka Elisabeth Miot-Noirault Winnie Deuther-Conrad Aurlie Maisonial-Besset 《Molecules (Basel, Switzerland)》2022,27(12)
Isocitrate dehydrogenases (IDHs) are metabolic enzymes commonly mutated in human cancers (glioma, acute myeloid leukaemia, chondrosarcoma, and intrahepatic cholangiocarcinoma). These mutated variants of IDH (mIDH) acquire a neomorphic activity, namely, conversion of α-ketoglutarate to the oncometabolite D-2-hydroxyglutarate involved in tumourigenesis. Thus, mIDHs have emerged as highly promising therapeutic targets, and several mIDH specific inhibitors have been developed. However, the evaluation of mIDH status, currently performed by biopsy, is essential for patient stratification and thus treatment and follow-up. We report herein the development of new radioiodinated and radiofluorinated analogues of olutasidenib (FT-2102) as tools for noninvasive single photon emission computed tomography (SPECT) or positron emission tomography (PET) imaging of mIDH1 up- and dysregulation in tumours. Nonradiolabelled derivatives 2 and 3 halogenated at position 6 of the quinolinone scaffold were synthesised and tested in vitro for their inhibitory potencies and selectivities in comparison with the lead compound FT-2102. Using a common organotin precursor, (S)-[125I]2 and (S)-[18F]3 were efficiently synthesised by radio-iododemetallation and copper-mediated radiofluorination, respectively. Both radiotracers were stable at room temperature in saline or DPBS solution and at 37 °C in mouse serum, allowing future planning of their in vitro and in vivo evaluations in glioma and chondrosarcoma models. 相似文献