• Title/Summary/Keyword: Benzophenone-3

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Tc-99m Labeling of Dione Bisoxime Compounds (Dione Bisoxime 계통의 화합물에 대한 테크네슘표지 원리에 관한 연구)

  • Jeong, Jae-Min;Cho, Jung-Hyuk;Oh, Seung-Joon;Lee, Myung-Chul;Chung, Soo-Wook;Chung, June-Key;Lee, Dong-Soo;Kwark, Cheol-Eun;Lee, Kyung-Han;Koh, Chang-Soon
    • The Korean Journal of Nuclear Medicine
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    • v.29 no.1
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    • pp.110-117
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    • 1995
  • Tc-99m Labeled hexamethylenepropyleneamineoxime ([$^{99m}Tc$]-HMPAO) is a famous amino-oxime compound and is widely used to construct SPECT images of cerebral blood flow. To investigate the relationship between chemical structure and radiolabeling in these kind of diamine-oxime compounds, we synthesized seven compounds by Schiff's base formation and successive reduction with sodium borohydride. They were (RR/SS )-4,8-diaza-3,6,6,9-tetramethylundecane-2,10-dione bisoxime (2), (RR/SS/meso)-4,8-diaza-3,9-dimethy-lundecane-2,10-dione bisoxime (4), (RR/SS/meso)-4,8-diaza-3,10-dimethyldodecane-2,11-dione bisoxime (5), (RR/SS/meso)-4,7-diaza-3,6,6,8-tetramethyldecane-2,9-dione bisoxime (8), (RR/SS/meso)-4,7-diaza-5,6-cyclohexyl-3,8-dimethyldecane-2,9-dione bisoxime (10), (RR/SS/meso)-3,4-bis(1-aza-2-methyl-3-oxime-1-butyl)-benzoic acid (12), and (RR/SS/ meso)-2,3-bis(1-aza-2-methyl-3-oxime-1-butyl) benzophenone (14). Chemical structures of all the synthesized compounds were identified by taking $^1H$ spectrum. Among them, 2 and 4 are propyleneamine oxime (PnAO), 6 is butyleneamine oxime (BnAO) and 8, 10, 12 and 14 are ethyleneamine oxime (EnAO). Each compound (0.5 mg) was incubated with stannous chloride (0.5 g - 8 g), carbonate-bicarbonate buffer (final concentration = 0.1 M, pH 7 - pH 10) and Tc-99m-pertechenate (1 ml). Tc-99m labeling of these compounds were checked by ITLC (acetone), ITLC (normal saline), reverse phase TLC (50 % acetonitrile) and ITLC (ethyl acetate). According to the results, EnAO's were not labeled by Tc-99m in any of above condition. About 11 % of maximum labeling efficiency was obtained with BnAO. However, 4 (PnAO) was labeled with Tc-99m to 85 % which is similar to the labeling efficiency of 2 (HMPAO). Hydrophilic impurity (9 % ) was the most significant problem with the labeling of 4, however, pertechnetate (3 % ) and colloid (3 %) were minor problem. In conclusion, we synthesized seven diamine blsoxlme compounds. Among them, four EnAO compounds were not labeled by Tc-99m. A BnAO was labeled poorly and two PnAO's were labeled well. These labeling can be explained by tertiary structure of their Tc-99m chelate.

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Changes in the Optical and Thermal Properties of Low-Temperature Cured Polyimide Thin Films Using the Catalyst (촉매를 이용한 저온경화 폴리이미드 박막의 광학적/열적 특성 변화)

  • Park, Myeong-Soon;Kim, Kwang-In;Nam, Ki-Ho;Han, Haksoo
    • Applied Chemistry for Engineering
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    • v.24 no.3
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    • pp.320-326
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    • 2013
  • In this study, various polyimide films were synthesized via low temperature cure in order to understand changes in their physical properties when using 4,4'-oxydianiline (ODA) as a diamine and dianhydride molecules with different backbones on a single diamine such as 4,4'-Oxydiphthalic anhydride (ODPA), 4,4-hexafluoroisopropylidene diphthalic dianhydride (6FDA), and 3,3', 4,4'-benzophenone tetracarboxylic dianhydride (BTDA). After the synthesis of poly(amic acid), polyimide films were fabricated by adding 1,4-diazabicyclo [2.2.2]octane (DABCO), a low-temperature catalyst, at various wt% to poly(amic acid)s. Changes of optical and thermal properties were compared and analyzed between polyimide films without catalyst and polyimide films with catalyst by FT-IR, UV-Vis transmittance, DSC/TGA, and WAXD analysis. Wide-angle X-ray diffraction (WAXD) analysis revealed that the mean intermolecular distance decreased with the use of a catalyst by the type of dianhydride. Thus, while the optical properties of the films improve by a low-temperature cure performed using a catalyst, their thermal properties decrease. These changes can be explained by the changes in the morphological structure of the films triggered by a catalyst-induced reduction in the mean intermolecular distance. Moreover, the results show that the type of dianhydride determines the degree of change in the optical and thermal properties in each types of polyimide, demonstrating that changes in the optical and thermal properties are directly associated with the backbone of the polyimide structure.

Weatherability of Organic-Inorganic Hybrid Coating Agents with N-Triethoxy silyl propyl quinine urethane (N-Triethoxy silyl propyl quinine urethane을 도입한 유-무기 복합 코팅제의 내후성)

  • Lee, Man Sung;Jo, Nam-Ju
    • Journal of Adhesion and Interface
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    • v.2 no.2
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    • pp.20-27
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    • 2001
  • Recently polycarbonate material has been utilized as windows in aircraft, buildings, and optical lens. However, while polycarbonate has excellent optical transparency, impact strength and many beneficial mechanical properties, it possesses poor abrasion resistance and weatherability. Then, there is a need for developing optically clear, anti-abrasive and weather resistant hard coating agents for polycarbonate. In this study, N-triethoxy silyl propyl quinine urethane(TESPQU) was synthesized with quinine and 3-isocyanato propyl triethoxy silane(3-IPTES). In order to introduce optically active silane in the main siloxane network, TESPQU was co-hydrolysed and co-condensed with methyl triethoxy silane(MTES) under acidic conditions. Polycarbonate sheets were coated with silica coating agents by the sol-gel method, and their abrasion resistance, ability of UV absorption and weatherability were evaluated. Coating agents containing hydroxybenzophenone as a UV absorber were also prepared to compare weatherability with TESPQU containing coating agent. TESPQU containing coating agent had good weatherability in accelerated QUV test.

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In vitro Acetolactate Synthase Inhibition of LGC-40863 in Rice and Barnyardgrass (시규제초제 LGC-40863의 벼와 피에 대한 Acetolactate synthase 저해 활성)

  • Bae, Y.T.;Lee, J.H.;Koo, S.J.
    • Korean Journal of Weed Science
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    • v.17 no.1
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    • pp.66-70
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    • 1997
  • LGC-40863(proposed common name ; pyribenzoxim), (benzophenone O-[2,6-bis[(4,6-dimethoxy-2-pyrimidinyl)oxy]benzoyl]oxime) is a new rice herbicide being developed by LG Chemical Ltd. The herbicide is highly selective between rice(Oryza sativa L.) and weeds including barnyardgrass (Echinochloa crus-galli(L.) P. Beauv.), and assumed to inhibit acetolactate synthase(ALS ; EC 4.1.3.18) because other structurally related herbicides inhibit the enzyme. To know inhibitory activity and the mode of inhibition of LGC-40863, $I_{50}$(concentration inhibiting ALS activity by 50%) and inhibition kinetics were investigated using ALS extracted from rice and barnyardgrass. $I_{50}$ values of LGC-40863 were 14 and 16mM in rice and barnyardgrass, respectively. In contrast to imazapyr(2-[4,5-dihydro-4-mythyl-4-(1-methylethyl)-5-oxo-1H-imidazol-2-yl]-3-pyridine-carboxylic acid) which showed an uncompetitive inhibition pattern, LGC-40863 was a noncompetitive inhibitor to ALS with respect to pyruvate similar to chlorsulfuron(2-chloro-N-((4-methoxy-6-methyl-l,3,5-triazin-2-yl) aminocarbonyl)benz-enesulfonamide) in both plants.

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Garcinol, an Acetyltransferase Inhibitor, Suppresses Proliferation of Breast Cancer Cell Line MCF-7 Promoted by 17β-Estradiol

  • Ye, Xia;Yuan, Lei;Zhang, Li;Zhao, Jing;Zhang, Chun-Mei;Deng, Hua-Yu
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.12
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    • pp.5001-5007
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    • 2014
  • The acetyltransferase inhibitor garcinol, a polyisoprenylated benzophenone, is extracted from the rind of the fruit of Garcinia indica, a plant found extensively in tropical regions. Anti-cancer activity has been suggested but there is no report on its action via inhibiting acetylation against cell proliferation, cell cycle progression, and apoptosis-inhibtion induced by estradiol ($E_2$) in human breast cancer MCF-7 cells. The main purposes of this study were to investigate the effects of the acetyltransferase inhibitor garcinol on cell proliferation, cell cycle progression and apoptosis inhibition in human breast cancer MCF-7 cells treated with estrogen, and to explore the significance of changes in acetylation levels in this process. We used a variety of techniques such as CCK-8 analysis of cell proliferation, FCM analysis of cell cycling and apoptosis, immunofluorescence analysis of NF-${\kappa}B$/p65 localization, and RT-PCR and Western blotting analysis of ac-H3, ac-H4, ac-p65, cyclin D1, Bcl-2 and Bcl-xl. We found that on treatment with garcinol in MCF-7 cells, $E_2$-induced proliferation was inhibited, cell cycle progression was arrested at G0/G1 phase, and the cell apoptosis rate was increased. Expression of ac-H3, ac-H4 and NF-${\kappa}B$/ac-p65 proteins in $E_2$-treated MCF-7 cells was increased, this being inhibited by garcinol but not ac-H4.The nuclear translocation of NF-${\kappa}B$/p65 in $E_2$-treated MCF-7 cells was also inhibited, along with cyclin D1, Bcl-2 and Bcl-xl in mRNA and protein expression levels. These results suggest that the effect of $E_2$ on promoting proliferation and inhibiting apoptosis is linked to hyperacetylation levels of histones and nonhistone NF-${\kappa}B$/p65 in MCF-7 cells. The acetyltransferase inhibitor garcinol plays an inhibitive role in MCF-7 cell proliferation promoted by $E_2$. Mechanisms are probably associated with decreasing ac-p65 protein expression level in the NF-${\kappa}B$ pathway, thus down-regulating the expression of cyclin D1, Bcl-2 and Bcl-xl.

Evaluation of Fungicides for Preventive and Curative Effects against Powdery Mildew on Oriental Melon (참외 흰가루병에 대한 살균제의 예방 및 치료효과 검정)

  • Chang, Tae-Hyun;Ryu, Yeon-Ju;Lim, Hye-Jung;Lim, Su-Jin;Choi, Mi-Young;Jeong, Byeong-Ryong;Kim, Cheol-Woong;Lee, Yong-Se
    • Korean Journal of Environmental Agriculture
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    • v.25 no.1
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    • pp.85-92
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    • 2006
  • Fungicides including keroxym-methyl (strobilurin fungicide), fenarimol and trifulmizole (DMI, boscalid (anilide) and metrafenone (benzophenone) were evaluated for preventive and curative efficacies against powdery mildew on oriental melon. The fungicides were applied preventatively at 7 days, 3 days and 3 hours before inoculation. Curative applications were made by applying fungicides three times at the interval of one week when infected leaves by powdery mildew were about 16% or 30%. Then preventative and curative efficacies were evaluated one week after inoculation and final application, respectively. Boscalid and metrafenone showed preventive efficacies of 74.3 and 68.3% against powdery mildew development respectively, when treated at 7 days before inoculation. They showed 89.4 and 87.2% efficacies when treated at 3 days before iniculation and 98.5 and 93.2% at 3 hours before inoculation respectively. However, there were no preventive efficacies in kresoxym-methyl, triflumizole and femarimol (DMI fungicides) when trebled at both 7 and 3 days before inoculation. At the preventive treatment 3 hours before inoculation, they indicated 59.0, 42.5, and 37.2% efficacies, respectively. When leaves were infected about 30% by powdery mildew, curative application of boscalid and metrafenone showed 85.9 and 74.0% of efficacies, respectively. Curative efficacies of kresoxym-methyl, tiflumizole and fernarimol were 5.5, 23.0 and 46.7% respectively. When leaves were infected about 16%, curative application of boscalid and metrafenone showed 100 and 97.5% of efficacies, respectively. However, the triflumizole and fernarimol showed relatively low curative efficacies of 30.8 and 51.6%, respectively. Microscopic observation of mycelial growth and conidia formation after detection of powdery mildew disease indicated lysis of mycelium and these lysis suppression of conidia formation showed tendency in accordance with curative efficacies of fungicides.