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Satoru Tamura Nobuhiro Shimizu Katsuaki Fujiwara Masafumi Kaneko Tominori Kimura Nobutoshi Murakami 《Bioorganic & medicinal chemistry letters》2010,20(7):2159-2162
Rational design by the MO calculation disclosed 5,6-dihydrovaltrate (2) as the bioisostere of valtrate (1), the Rev-export inhibitor with anti-HIV activity. The synthesis of 2 was accomplished by ingenious use of asymmetric Diels–Alder reaction and stereoselective epoxidation associated with the adjacent hydroxyl group. Because of similar biological potency to 1, the analog 2 should be recognized as a promising scaffold for new anti-HIV agents with an unprecedented mechanism of action, inhibition for nuclear export of Rev protein, in the conventional remedy. 相似文献
3.
Mitsuaki Yamashita Masafumi Kaneko Harukuni Tokuda Katsumi Nishimura Yuko Kumeda Akira Iida 《Bioorganic & medicinal chemistry》2009,17(17):6286-6291
A series of naphthoquinones based on the naphtho[2,3-b]furan-4,9-dione skeleton such as (−)-5-hydroxy-2-(1′-hydoxyethyl)naphtho[2,3-b]furan-4,9-dione (1) and its positional isomer, (−)-8-hydroxy-2-(1′-hydoxyethyl)naphtho[2,3-b]furan-4,9-dione (2), which are secondary metabolites found in the inner bark of Tabebuia avellanedae, were stereoselectively synthesized and their biological activities were evaluated in conjunction with those of their corresponding enantiomers. Compound 1 exhibited potent antiproliferative effect against several human tumor cell lines, but its effect against some human normal cell lines was much lower than that of mitomycin. On the other hand, its enantiomer (R)-1 was less active toward the above tumor cell lines than 1. The antiproliferative effect of 2 against all tumor cell lines was significantly reduced. These results indicated the presence of the phenolic hydroxy group at C-5 is of great important for increasing antiproliferative effect. In addition, 1 also showed higher cancer chemopreventive activity than 2, while there were no significant differences between 1 and 2 in antimicrobial activity. Both compounds displayed modest antifungal and antibacterial activity (Gram-positive bacteria), whereas they were inactive against Gram-negative bacteria. 相似文献
4.
Masafumi Komiya Shigehiro Asano Nobuyuki Koike Erina Koga Junetsu Igarashi Shogo Nakatani Yoshiaki Isobe 《Bioorganic & medicinal chemistry》2012,20(23):6840-6847
Based on 2-(4-phenoxybenzoyl)-5-hydroxyindole (2), a novel structural class of CaMKII inhibitors were synthesized and further optimized. The strong acidity of the hydroxyl group and the lipophilic group at the 4 and 6-positions were found to be necessary for strong CaMKII inhibition. Compound 25 was identified as a promising compound with 50-fold more potent inhibitory activity for CaMKII than 2. Compound 25 also showed high selectivity for CaMKII over off-target kinases. 相似文献
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6.
To estimate the water status of Hinoki cypress (Chamaecyparis obtusa) under reduced hydraulic conductance, we measured diurnal changes in the trunk diameter of two 20-year-old trees during a hot dry summer. One tree showed a greatly reduced water-transport area in its trunk cross-section and leaf specific hydraulic conductivity. Diurnal changes in trunk diameter were measured at the xylem surface using a strain-gauge method. At the start of the experiment, the diurnal changes in trunk diameter were similar in both trees with shrinking during the day and swelling at night. However, in the trunk of the tree with reduced hydraulic conductance, the maxima and minima decreased rapidly as days passed. These differences in trunk diameter changes might be caused by the differences in the leaf-specific hydraulic conductance. 相似文献
7.
At least three regulatory elements GPE1, GPE2 and GPE3 (G-CSF promoter elements) controlling the gene (G-CSF) encoding granulocyte colony-stimulating factor (G-CSF) are indispensable for the constitutive expression of the G-CSF gene in human CHU-2 cells and for its lipopolysaccharide(LPS)-inducible expression in macrophages. The enhancer activities of each regulatory element were examined with or without the SV40 enhancer element placed downstream from the reporter gene. A GPE1 tetramer mediated the constitutive expression in CHU-2 cells, and the LPS-inducible expression in macrophage cell lines, while the GPE2 element was active in CHU-2 and LPS-treated macrophage cell lines only in combination with the SV40 enhancer. A GPE3 tetramer had efficient enhancer activity in CHU-2 cells but not in macrophage cell lines without the SV40 enhancer. In combination with the SV40 enhancer, GPE3 worked as an LPS-inducible enhancer element in macrophage BAM3 cells. Gel retardation assay indicated that the CHU-2 and the macrophage cells contained nuclear factors which specifically bound to each GPE sequence. 相似文献
8.
Aina Gotoh Masafumi Hidaka Keiko Hirose Takafumi Uchida 《The Journal of biological chemistry》2013,288(48):34699-34706
Neurons undergo several morphological changes as a part of normal neuron maturation process. Alzheimer disease is associated with increased neuroproliferation and impaired neuronal maturation. In this study, we demonstrated that Gas7b (growth arrest specific protein 7b) expression in a neuronal cell line, Neuro 2A, induces cell maturation by facilitating formation of dendrite-like processes and/or filopodia projections and that Gas7b co-localizes with neurite microtubules. Molecular analysis was performed to evaluate whether Gas7b associates with actin filaments and microtubules, and the data revealed two novel roles of Gas7b in neurite outgrowth: we showed that Gas7b enhances bundling of several microtubule filaments and connects microtubules with actin filaments. These results suggest that Gas7b governs neural cell morphogenesis by enhancing the coordination between actin filaments and microtubules. We conclude that lower neuronal Gas7b levels may impact Alzheimer disease progression. 相似文献
9.
Norihide Hinomoto Tomomi Higaki Junichiro Abe Masafumi Yamane Eizi Yano 《Applied Entomology and Zoology》2012,47(2):165-171
We have developed and characterized 21 microsatellite markers in the aphidophagous gall midge Aphidoletes aphidimyza (Rondani) (Diptera: Cecidomyiidae). All 21 loci tested were polymorphic: the number of alleles ranged from 2 to 17. Allelic
richness and observed heterozygosities were higher in females than in males. Several loci had no heterozygosity in males,
suggesting that the loci were located on sex chromosomes or E-chromosomes, common to cecidomyiids. The high polymorphism detected
in this study suggests the markers will be of value in analyzing genetic structure of field populations. 相似文献
10.