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81.
Inhibition of Metalloproteinase Activity by Chinese Formulations Used to Treat Inflammatory Diseases
JIN Feng-hai WANG Hui-ling ZHAO Shu-hua YANG Jin-gang FANG Xue-xun 《高等学校化学研究》2006,22(2):245-247
Introduction Matrixmetalloproteinases(MMPs)areaclassof zinc requiringextracellularendopeptidasesthatcanto getherdegradeallcomponentsoftheextracellularma trixandbasementmembranes[1—3].Theyplayimpor tantrolesinconnectivetissueremodeling,occurringin normalb… 相似文献
82.
83.
Ilya I. Moiseev Tatiana A. Stromnova Irina N. Busygina Natalya Yu. Tihonova Natalya Yu. Kozitsyna Arkady M. Ellern Mikhail Yu. Antipin Yury T. Struchkov 《Journal of Cluster Science》1992,3(4):411-421
Thermolysis of tetranuclear palladium clusters Pd4(-Q)4 Pd4(-Q)4(-O2CR)4 (Q=CPh2 or CO;R=Me, CMe3, Ph, CH2Cl or CF3) has been found to involve innersphere oxidation of carbene or carbonyl ligands during which an oxygen atom transfer occurs from the carboxylate group to the carbene or carbonyl ligand. The thermolysis of the carbonyl clusters gives rise to the products of CO2 insertion into the C–H bond of benzene or toluene used as solvents forming benzoic acid from benzene and a mixture of phenylacetic and toluic acids from toluene. The reaction of [Pd(OAc)2(PPh3)]2 with HCO2H includes the transfer of an O atom from formate ligand to the P atom and cleavage of the P-Ph bond accompanied by transfer of the Ph group from PPh3 ligand to the palladium atom. The structure of the complex formed, [Pd(-O2PPh2)(C6H5)(PPh3)]2, has been resolved by X-ray analysis. 相似文献
84.
Simanenko Yu. S. Popov A. F. Prokop'eva T. M. 《Theoretical and Experimental Chemistry》2003,39(5):288-295
Among hydroxamate ions (typical nucleophiles), anomalously high nucleophilicity relative to 4-nitrophenyl diethyl phosphonate is seen in anions which have general basic catalytic sites that provide anchimeric assistance for proton transfer in the transition state. 相似文献
85.
86.
Ana Montero 《Tetrahedron letters》2005,46(3):401-405
A stereocontrolled synthesis of an unsaturated sugar bearing two amino groups (one of them masked as an azide), using an Overman rearrangement as key step, is described. This scaffold is used to prepare two peptides having aromatic fragments, which have shown activity as calpain inhibitors. 相似文献
87.
Akiko Saito Mana Emoto Akira Tanaka Yuki Doi Kazuaki Shoji Yoshiyuki Mizushina Hiroshi Ikawa Hiromi Yoshida Nobuyasu Matsuura Noriyuki Nakajima 《Tetrahedron》2004,60(52):12043-12049
A simple method for the synthesis of procyanidin B3 substituted with a galloyl group at the 3 and 3″ position is described. Condensation of a benzylated catechin-3-O-gallate electrophile with a nucleophile, catechin and catechin-3-O-gallate, proceeded smoothly and stereoselectively to afford the corresponding dimer gallates, procyanidin B3-3-O-gallate and procyanidin B3-3,3″-di-O-gallate, in good yields. Further, their antioxidant activities on UV-induced lipid peroxide formation, DPPH radical scavenging activity and inhibitory activity of DNA polymerase were also investigated. Among three procyanidin B3 congeners (procyanidin B3, 3-O-gallate and 3,3″-di-O-gallate), the 3,3″-di-O-gallate derivative showed the strongest antioxidant and radical scavenging activity. Interestingly, the 3-O-gallate derivative was the strongest inhibitor of mammalian DNA polymerase with IC50 value of 0.26 μM, although it showed the weakest antioxidant and radical scavenging activity. It became apparent that the presence of a galloyl group at the C-3 position in the proanthocyanidin oligomer was very important for biological activity, however, the antioxidant activity of these compounds was not parallel to the DNA polymerase inhibitory activity. 相似文献
88.
PEPAMP是应用于工业循环水中的新一代高效阻垢剂.采用电喷雾电离质谱和质谱/质谱技术分析了合成产物,注射泵直接进样,正离子方式检测,方法简便、快速.通过EI-MS技术获得了目标产物PEPAMP及主要副产物的准分子离子峰,通过ESI-MS-MS技术获得了其碎片信息,并对目标化合物及主要副产物进行了精确质量测定,确定了目标化合物及主要副产物的结构. 相似文献
89.
Chao Zhang 《Tetrahedron》2007,63(26):5832-5838
The ability to inhibit any protein kinase of interest with a small molecule is enabled by a combination of genetics and chemistry. Genetics is used to modify the active site of a single kinase to render it distinct from all naturally occurring kinases. Next, organic synthesis is used to develop a small molecule, which does not bind to wild-type kinases but is a potent inhibitor of the engineered kinase. This approach, termed chemical genetics, has been used to generate highly potent mutant kinase-specific inhibitors based on a pyrazolopyrimidine scaffold. Here, we asked if the selectivity of the resulting pyrazolopyrimidines could be improved, as they inhibit several wild-type kinases with low-micromolar IC50 values. Our approach to improve the selectivity of allele-specific inhibitors was to explore a second kinase inhibitor scaffold. A series of 6,9-disubstituted purines was designed, synthesized, and evaluated for inhibitory activity against several kinases in vitro and in vivo. Several purines proved to be potent inhibitors against the analog-sensitive kinases and exhibited greater selectivity than the existing pyrazolopyrimidines. 相似文献
90.
Wolfgang Benetka Manfred Koranda Frank Eisenhaber 《Monatshefte für Chemie / Chemical Monthly》2006,137(10):1241-1281
Summary. Since 1979, when prenylation has been first discovered as chemical oddity of a yeast mating factor, the two forms of this
posttranslational modification of proteins (farnesylation and geranylgeranylation) have been found as wide spread among proteins
from Eukarya and their viruses. This review attempts to summarize as comprehensively as possible the enzymological processes
of prenylation and the various aspects of their biological significance.
The substrate proteins of prenyltransferases are known to carry a sequence signal composed of a cysteine-containing 4–5 residue
stretch at the utmost C-terminal end that is N-terminally preceded by a flexible and polar linker region of ca. 10 residues. Postprenylation processing of substrate proteins can involve C-terminal proteolysis, C-terminal carboxyl methylation,
and other steps of maturation. The prenyl anchor functions as module for membrane attachment or for protein–protein interaction.
Prenyl anchor carrying proteins fulfill a large array of functions in signaling and regulation of cellular processes. Therefore,
they are involved in the pathogenesis of a variety of human diseases, the most prominent one being cancer. Farnesyltransferase
inhibitors show surprisingly high efficiency in controlling tumor growth in model systems but, so far, clinical trials with
human patients have remained without the desired success. Interference into prenylation pathways appears also a promising
treatment principle in a variety of parasitic diseases. 相似文献