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101.
Integrin ligands containing the tripeptide sequences Arg-Gly-Asp (RGD) and iso-Asp-Gly- Arg (isoDGR) were actively investigated as inhibitors of tumor angiogenesis and directing unit in tumor-targeting drug conjugates. Reported herein is the synthesis, of two RGD and one isoDGR cyclic peptidomimetics containing (1S,2R) and (1R,2S) cis-2-amino-1-cyclopentanecarboxylic acid (cis-β-ACPC), using a mixed solid phase/solution phase synthetic protocol. The three ligands were examined in vitro in competitive binding assays to the purified αvβ3 and α5β1 receptors using biotinylated vitronectin (αvβ3) and fibronectin (α5β1) as natural displaced ligands. The IC50 values of the ligands ranged from nanomolar (the two RGD ligands) to micromolar (the isoDGR ligand) with a pronounced selectivity for αvβ3 over α5β1. In vitro cell adhesion assays were also performed using the human skin melanoma cell line WM115 (rich in integrin αvβ3). The two RGD ligands showed IC50 values in the same micromolar range as the reference compound (cyclo[RGDfV]), while for the isoDGR derivative an IC50 value could not be measured for the cell adhesion assay. A conformational analysis of the free RGD and isoDGR ligands by NMR (VT-NMR and NOESY experiments) and computational studies (MC/EM and MD), followed by docking simulations performed in the αVβ3 integrin active site, provided a rationale for the behavior of these ligands toward the receptor.  相似文献   
102.
The title mol­ecule, 2′‐pyrenyl­spiro­[2,3‐di­hydro‐1H‐cyclo­penta­[b]­naphthalene‐2,5′‐1′,3′‐dioxane]‐4,9‐dione, C32H22O4, contains an electron‐donating pyrene group spiro‐linked to an electron‐accepting naphtho­quinone. The mol­ecules are V‐shaped in profile and stack to form columns along b with alternating, approximately coplanar, pyrene and naphtho­quinone fragments. Intermolecular contacts within a column are consistent with some degree of π contact and possible long‐range delocalization. Individual columns form a herringbone pattern when the crystal is viewed along b .  相似文献   
103.

Background  

It is well known that both semantic and syntactic information play a role in pronoun resolution in sentences. However, it is unclear what the relative contribution of these sources of information is for the establishment of a coreferential relationship between the pronoun and the antecedent in combination with a local structural case constraint on the pronoun (i.e. case assignment of a pronoun under preposition governing). In a prepositional phrase in German and Dutch, it is the preposition that assigns case to the pronoun. Furthermore, in these languages different overtly case-marked pronouns are used to refer to male and female persons. Thus, one can manipulate biological/syntactic gender features separately from case marking features.  相似文献   
104.
In the search of new natural products to be explored as possible anticancer drugs, two plant species, namely Ononis diffusa and Ononis variegata, were screened against colorectal cancer cell lines. The cytotoxic activity of the crude extracts was tested on a panel of colon cancer cell models including cetuximab-sensitive (Caco-2, GEO, SW48), intrinsic (HT-29 and HCT-116), and acquired (GEO-CR, SW48-CR) cetuximab-resistant cell lines. Ononis diffusa showed remarkable cytotoxic activity, especially on the cetuximab-resistant cell lines. The active extract composition was determined by NMR analysis. Given its complexity, a partial purification was then carried out. The fractions obtained were again tested for their biological activity and their metabolite content was determined by 1D and 2D NMR analysis. The study led to the identification of a fraction enriched in oxylipins that showed a 92% growth inhibition of the HT-29 cell line at a concentration of 50 µg/mL.  相似文献   
105.
106.
Microwave heating of ceramic composites   总被引:1,自引:0,他引:1  
The microwave heating of a ceramic composite is modelled andanalysed. The composite consists of many small ceramic particlesembedded in a ceramic cement. The composite is assumed to bewell insulated, and each particle is assumed to be in imperfectthermal contact with the surrounding cement. Based on thesetwo assumptions an asymptotic theory exploiting the small Biotnumber and small non-dimensional contact conductance is developed.Our asymptotic theory yields a set of nonlinear partial differentialequations which govern the temperature in the composite. Theseare reduced to a set of coupled nonlinear ordinary differentialequations in which the surface area of each particle entersas a parameter. Recent experiments with such composites haveshown that the steady-state temperature of the composite isstrongly dependent upon the radii of the embedded particles.Our model captures this effect. In fact, our analysis showsthat the assumption of imperfect thermal contact between theparticles and the ceramic cement is essential for this trendto be established.  相似文献   
107.
108.
TiCl4 mediated aldol condensations establish multiple contiguous chiral centers in an almost complete enantio- and diastereoselective way.  相似文献   
109.
Catechol boron halides (1,X=Cl, Br) cleave certain ether, ester and carbamate protecting groups under mild conditions. The scope and selectivity of these readily available reagents has been examined.  相似文献   
110.
ICP-AES法测定色漆可溶性金属含量   总被引:1,自引:0,他引:1  
用ICP-AES法测定了色漆中的“可溶性”金属铬、镉、铅元素,考察了不同酸度对分析结果的影响,优化了测试条件。进行了回收率和精密度试验。并用原子吸收光谱国标方法进行对照,结果一致。  相似文献   
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