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41.
42.
Tetsuo Suami Hiroaki Sasai Kazuhiro Matsuno Nobuo Suzuki Yoshimasa Fukuda Osamu Sakanaka 《Tetrahedron letters》1984,25(40):4533-4536
Tunicamycins and their eight analogs have been synthesized by condensation of a N-acetyl-D-glucosamine derivative and an anomeric chloride of tunicaminyl uracil, followed by deprotections and N-acylation. 相似文献
43.
Two new phenolic compounds, glicoricone (3) and licofuranone (4), were isolated from a species of licorice brought from the northwestern region of China, and their structures were assigned. Among the twelve licorice constituents examined for the inhibition of monoamine oxidase (MAO), six compounds, 3, 4, genistein (6), licopyranocoumarin (7), licocoumarone (14) and glycyrrhisoflavone (15), inhibited the enzyme with the IC50 (concentration required for 50% inhibition of the enzyme activity) values of 6.0 x 10(-5)-1.4 x 10(-4) M. Glycyrrhizin (1) also inhibited MAO with the IC50 value of 1.6 x 10(-4) M. 相似文献
44.
Norio Miyoshi Kiyoaki Hara Issei Yokoyama Giiti Tomita Masaru Fukuda 《Photochemistry and photobiology》1988,47(5):685-688
Abstract— The absorption and fluorescence spectra, and the fluorescence lifetime of acridine orange (AO) were measured in a wide range of the sodium dodecyl sulfate (SDS) concentration below and above the critical micelle concentration (cmc). The fluorescence consisted of two components with different lifetimes; short (<3 ns) and long (>3 ns). The short and long lifetime components are attributed to the AO monomer and dimer associated with detergent, respectively. The lifetime of the dimer increased with increasing the SDS concentration just below the cmc. It decreased suddenly to a constant value just above the cmc. The lifetime of the monomer showed only a slight increase in the concentration range of SDS employed. 相似文献
45.
The stability constants of the ternary complexes containing UTP, 2,2′-bipyridyl (bipy), and Co2+, Ni2+, Cu2+, or Zn2+ (M2+) have been determined by potentiometric titrations (Table 1). Changes in stability are quantified by Δlog KM = log K–log K. For the Co2+, Ni2+, Cu2+, and Zn2+ systems Δlog KM is 0.10, ?0.13, 0.36, and 0.15, respectively. All these ternary complexes are considerably more stable than would be expected on statistical grounds; indeed, for Co2+, Cu2+, and Zn2+, UTP4? binds more tightly to M (bipy)2+ than to M2+. An UV. difference spectroscopic study suggests that stacked adducts between bipyridyl and the pyrimidine moiety of uridine are formed. 1H-NMR. studies of the bipy/uridine, bipy/UTP, and bipy/UTP/Zn2+ systems (Figs. 1 and 2) confirm the presence of stacking in the binary adducts and in the ternary complex. There is also evidence for the existence of the stacked protonated complex, Zn(bipy) (HUTP)?, with the proton at the γ-phosphate group. The acidity constant of this ternary complex has been measured (Fig. 3). The observed stability enhancement of stacked adducts by the formation of a metal ion bridge is discussed (Fig. 4) and biological implications are indicated. 相似文献
46.
C-H to N substitution dramatically alters the sequence-specific DNA alkylation, cytotoxicity, and expression of human cancer cell lines 总被引:2,自引:0,他引:2
Bando T Narita A Iwai A Kihara K Sugiyama H 《Journal of the American Chemical Society》2004,126(11):3406-3407
We designed and synthesized sequence-specific alkylating conjugates 1 and 2, which selectively alkylate matched sequences at nanomolar concentrations. Conjugates 1 and 2 differ only in that the C-H is substituted by an N in the second ring, which precisely recognizes and effectively alkylates DNA according to the recognition rule of Py-Im polyamides. We investigated sequence-specific DNA alkylation, cytotoxicity in 39 human cancer cell lines, and the effect on expression levels in cancer cell lines by Py-Im conjugates 1 and 2. The COMPARE analysis of the mean graphs showed that conjugates 1 and 2 did not correlate well with each other (r = 0.65) despite having a common DNA alkylating mechanism (purine N3 alkylation). Array-based gene expression analysis demonstrated that there are several oppositely regulated genes. The results suggest the intriguing possibility that DNA alkylating agents recognizing longer base-pair sequences may provide a promising approach for developing new types of antigene agents. 相似文献
47.
The Grignard coupling of 2,2-dibromo-1-phenyladamantane gave trans-2,2'-bi(1-phenyladamantylidene) (1-Ph). Single-crystal X-ray analysis indicated that 1-Ph has a 23.2 degrees twisted double bond, which is much more distorted than that of parent 2,2'-biadamantylidene (1-H) and that of the ethyl-substituted derivative (1-Et). A cyclic voltammogram showed a reversible electron oxidation wave at 0.87 V vs Fc/Fc(+), which is 0.19 V lower than 1-H, indicating a significant increase in the HOMO energy level due to the distortion. The reaction of 1-Ph with 0.9 equiv of bromine gave an intramolecular Friedel-Crafts alkylation product, while bromination of 1-H and 1-Me has been reported to give a bridged bromonium ion and a rearranged product, 2-(1-methyl-2-adamantylidene)-4-bromotricyclo[5,3,1,0(3.9)]undec-4-ene, respectively. 相似文献
48.
H. Sakurai M. Fukuda Y. Hayashibe Y. Sayama K. Masumoto T. Ohtsuki 《Journal of Radioanalytical and Nuclear Chemistry》1997,217(2):267-271
A highly sensitive determination of fluorine in standard rocks by photon activation using the19F(,n)18F reaction combined with pyrohydrolysis for the separation of18F has been reported. The irradiation energy was operated at 20 MeV to avoid the interference from Na, because Na is one of the major element in rocks and18F is also produced from Na via23Na(,n)18F reaction above its threshold energy, 20.9 MeV. After irradiation, fluorine was extracted by pyrohydrolysis and separated as LaF3 precipitate. It was ascertained that the average recovery of fluorine in standard rocks was about 90% and the precipitate was of high radiochemical purity. This method was applied to the analysis of ten GSJ rock reference samples and two USGS standard rocks issued by the Geological Survey of Japan and the United States Geological Survey, respectively. The detection limit of this method was 0.02 g/g, and the results obtained by this method were in good agreement with the recommended values. This method was easily applied to the determination of a few ppm level of fluorine in rock samples, such as ultrabasic rock and feldspar. 相似文献
49.
Ryuichi Iemura Tsuneo Kawashima Toshikazu Fukuda Keizo Ito Goro Tsukamoto 《Journal of heterocyclic chemistry》1987,24(1):31-37
Several types of benzimidazole derivatives were prepared and were screened for H 1-antihistaminic activity. Most of the compounds showed potent antihistaminic activity in vitro. Among them 2-[(1-piperazinyl)methyl]-benzimidazoles 14 and 2-[(1-homopiperazinyi)methyl]benzimidazoles 15 exhibited potent activity also in vivo. 相似文献
50.
T Kawakita T Kuroita M Yasumoto M Sano K Inaba T Fukuda T Tahara 《Chemical & pharmaceutical bulletin》1992,40(3):624-630
A series of 3,4-dihydro-3-oxo-1,4-benzoxazine-8-carboxamide derivatives was synthesized and evaluated for serotonin-3 (5-HT3) receptor antagonistic activity assessed by their ability to antagonize the von Bezold-Jarish (BJ) effect in rats. Derivatives bearing 1-azabicyclo[2.2.2]oct-3-yl moiety as a basic function attached to the carboxamide at position 8 showed more potent antagonistic activity than those bearing the other three basic moieties. Structure-activity relationships of this series showed that methyl and chloro groups were more effective as substituents at positions 4 and 6, respectively. The representative compound 15 (Y-25130) in this series showed potent antagonistic activity on the BJ effect (ED50 = 1.3 micrograms/kg i.v.), high affinity for 5-HT3 receptor (Ki = 2.9 nM) and complete protection against cisplatin-induced emesis in dogs at a dose of 0.1 mg/kg i.v. 相似文献