• YAKHAK HOEJI
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• v.31 no.5
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• pp.338-342
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• 1987

8-tert-Butyl-6,7-dihydro-5-methyl-8H-pyrrolo [3,2-e]-s-triazolo [1,5-a] pyrimidine (Bumepidil), one of the s-triazolo [1,5-a] pyrimidine derivatives, has been recently found to be the most promising potential coronary vasodilator and antihypertensive agent. In this report, a new synthetic approach for Bumepidil, via direct N-amination of amino pyrimidine intermediate, was studied and found to be useful method. The novel synthetic method comprise the following steps, acylation of $\gamma$-butyrolactone, condensation with guanidine, direct N-amination, cyclization, chlorination, and finally cyclization using tert-butyl amine.

• Journal of the Korea Society of Computer and Information
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• v.28 no.5
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• pp.9-15
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• 2023

In this paper, we propose a method predicting the speed of each lane from the link speed using a neural network. We took three measures for configuring learning data to increase prediction accuracy. The first one is to expand the spatial range of the data source by including 14 links connected to the beginning and end points of the link. We also increased the time interval from 07:00 to 22:00 and included the data generation time in the feature data. Finally, we marked weekdays and holidays. Results of experiments showed that the speed error was reduced by 21.9% from 6.4 km/h to 5.0 km/h for straight lane, by 12.9% from 8.5 km/h to 7.4 km/h for right turns, and by 5.7% from 8.7 km/h to 8.2 km/h for left-turns. As a secondary result, we confirmed that the prediction accuracy of each lane was high for city roads when the traffic flow was congested. The feature of the proposed method is that it predicts traffic conditions for each lane improving the accuracy of prediction.

• KSBB Journal
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• v.10 no.5
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• pp.568-574
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• 1995

To investigate the effect of pH on organic acid production by Anaerobiospirillum succiniciproducens, an anaerobic fermentation was carried out by maintaining the pH of the fermentation broth at 5.8, 6.0, 6.4, 6.8, and 7.2. At various pHs, the concentrations of cell were $1.0∼1.9g/\ell$ which were two to three times higher than those of the other worker's results, and the maximum was obtained at pH 5.8. Substrate consumption was increased by increasing the pH in the range of pH 6.0 to 6.8, while the sugar consumption rate at both pH 5.8 and 7.2 was very slow. The total amount of 2M $Na_2C0_3$ added for adjustment of pH change due to organic acid production was maximum at pH 6.8. Changes of conductivity of the fermentation broth was very simillar to those of 2M $Na_2C0_3$ added at various pHs. Therefore, it is suggested that determination of the amount of organic acid in a broth can be possible by measuring the conductivity. The maximum production yield of lactate based on glucose was 64% for pH 7.2 and 32% for pH 6.8, respectively.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.9
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• pp.4101-4107
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• 2014

Protein phosphatase 1 (PP1) is a major serine/threonine phosphatase that controls gene expression and cell cycle progression. The active mutant IPP5 ($8-60hIPP5^m$), the latest member of the inhibitory molecules for PP1, has been shown to inhibit the growth of human cervix carcinoma cells (HeLa). In order to elucidate the underlying mechanisms, the present study assessed overexpression of $8-60hIPP5^m$ in HeLa cells. Flow cytometric and biochemical analyses showed that overexpression of $8-60hIPP5^m$ induced G2/M-phase arrest, which was accompanied by the upregulation of cyclin B1 and phosphorylation of G2/M-phase proteins ATM, p53, $p21^{cip1/waf1}$ and Cdc2, suggesting that $8-60hIPP5^m$ induces G2/M arrest through activation of the ATM/p53/$p21^{cip1/waf1}$/Cdc2/cyclin B1 pathways. We further showed that overexpression of $8-60hIPP5^m$ led to delayed nuclear translocation of cyclin B1. $8-60hIPP5^m$ also could translocate to the nucleus in G2/M phase and interact with $pp1{\alpha}$ and Cdc2 as demonstrated by co-precipitation assay. Taken together, our data demonstrate a novel role for $8-60hIPP5^m$ in regulation of cell cycle in HeLa cells, possibly contributing to the development of new therapeutic strategies for cervix carcinoma.

• KSBB Journal
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• v.14 no.1
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• pp.58-65
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• 1999

A hydrogel, poly(N-isopropylacrylamide-co-N,N'-dimethylaminopropyl methacrylamide), sensitive to both pH and temperature was synthesized and characterized for its welling behavior, lower critical solution temperature (LCST), and its appearance. The hydrogel with 5 mol% of N,N'-diemthylaminopropyl methacrylamide (DMAPMAAm) increased its volume phenomenonally in a lower pH range (ph 1~8) even at temperature ($37^{\circ}C$ and $40^{\circ}C$) higher than LCST. This behavior was unique compared to the temperature -sensitive hydrogel which did not exhibit any swelling in the same pH range. The hydrogel with 20 mol% of DMAPMAAm was swollen significantly at a higher pH of 12. With pH decrease from 12 to 2 water content in the gel increased from 38.8 wt% and 60.6 wt%, and 90.8 wt% for 5 mol% and 20 mol% gel, respectively. The transition pH that pH effect overwhelmed temperature effect occurred at a lower pH for a higher temperature ($40^{\circ}C$) and a lower mol% (5 mol%) of DMAPMAAm. Transparency and LCST of the gel increased with higher DMAPMAAm mol%.

• Korean Journal of Microbiology
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• v.29 no.6
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• pp.387-391
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• 1991

Methylobacterium extorquens AM1 growing on methanol as a sole source of carbon and energy was found to grow most rapidly (t$t_{d}$ =6h) at 30.deg.C in a mineral medium (pH 7.0) containing 0.5% (v/v) methanol which was agitated at 200 rpm (optimal cultivation condition). Cells grown under the optimal cultivation condition contained more spermidine, but less putrescine, than the cells grown on 2.5%(v/v) ( $t_{d}$ =8h ) or at 20.deg.C ( $t_{d}$ =8h ). Cells cultivated under the optimal condition was found to contain more spermidine than the cells grown at pH 6.0 (( $t_{d}$ =7h ) and pH 8.0 ($t_{d}$ =7.3h). the cells growing at the stationary phase under the optimal condition accumulated more spermine or putrescine than the cells growing at the same phase on 2.5%(v/v) methanol or at pH 6.0 and pH 8.0, respectively. M. extorquens AM1 grown in a medium agitated at 100 rpm ( $t_{d}$ =8.8h ) contained less spermidine and spermine than the cells grown under the optimal cultivation condition.

• Journal of the Korean Chemical Society
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• v.19 no.2
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• pp.92-97
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• 1975

The molecular and electronic structures of $TiCl(OC_6H_5)_3{\cdot}C_6H_5OH\;and\;Ti(OC_6H_5)_4{\cdot}C_6H_5OH$ have been studied by employing cryoscopic and electronic spectroscopic methods. The cryoscopic data have shown that the dimeric tetraphenoxytitanium(Ⅳ) phenolate in solid undergoes complete dissociation into monomer in solution and also the chlorocomplex starts dissociation around the concentration of 8 m mole/l. Therefore, these two Ti-complexes are pentacoordinated in dilute solution and the local symmetry of the titanium ion in these complexes seems to be trigonalbipyramid. The electronic spectra of $TiCl(OC_6H_5)_3{\cdot}C_6H_5OH$ and $Ti(OC_6H_5)_4{\cdot}C_6H_5OH$ each show two band, systems, one vibration-structural band characteristic of the aromatic ring in the near UV and another visible band at 26.8 kK, 29.6 kK, respectively, which are assigned as a ligand to metal charge transfer band corresponding to $^1A_1''{\to}^1E'\;or\;^1E''$ transition.

• Archives of Pharmacal Research
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• v.24 no.5
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• pp.390-396
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• 2001

Synthesized 6-arylamino-5,8-quinolinediones 4a-4j and 6-chloro-7-arylamino-5,8-isoquinolinediones 5a-5g were evaluated for effects on NAD(P)H quinone oxidoreductase (NQOl ) activity with the cytosolic fractions derived from cultured human lung cancer cells and their cytotoxicity in cultured several human solid cancer cell lines. The 5,8-quinolinediones 4 and 5,8-isoquinolinediones 5 affected the reduction potential by NQO1 activity and showed a potent cytotoxic activity against human cancer cell lines. The tested compounds 4a, 5c, 5f, and 5g were considered as more potent cytotoxic agents. The compounds 4d, 5b, 5c, 5e and 5g were comparable modulators of NQO1 activity.

• Parasites, Hosts and Diseases
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• v.27 no.3
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• pp.161-170
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• 1989

The proteases of Toxoplasma gcndii were purified partially and characterisrd for some biochemical properties including various chromatographic patterns, major catalytic classes, and conditions to promote the activity of these enzymes. When Toxoplasma extract was incubated with 3H-casein at various pH, peak hydrolysis of casein was observed at pH 6.0 and at pH 8.5. Proteasfs working at pH 6.0 and at pH 8.5 were purified partially by conventional methods of chromatographies of DE52 anion rxchange, Sephadex G-200 gel permeation, and hydroxylapatite chromatography. Partially purified enzymes were tested by site-specific inhibitors and promotorf. The protease working at pH 6.0 was inactivated by iodoacetamide with LDso of 10-5 M and promoted by dithiothreitol, while the protease working at pH 8.5 was inhibited by phenylmethylsulfonyl fluoride with LD50 of 10-5 M and was Promoted by ATP (excess ATP beyond 2 mM inhibited the activity reversely). The protease of pH 8.5 had the activity of ATPase which might exert the energy to its action. Therefore the former was referred to as a cysteinyl acid protease and the latter, ATP-dependent neutral serine protease.

• YAKHAK HOEJI
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• v.41 no.2
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• pp.181-186
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• 1997

A series of 7-deazahypoxanthine and 7-deazaadenine derivatives[6,7.8.9.10,13] as purine antagonists was prepared. The pyrrolidine-5-one derivatives[4,11] were treated vith $(C_2H_5)_3OBF_4$ to give 3- aryl-5-ethoxy-2H-3,4-dihydropyrrole[5,12], which were converted to 7-aryl-7,8-dihydro-7(9H)-deazahy-poxanthine[6,7,8,9,10] and 7-phenyl-2-methyl-7,8- dihydro-7(9H)-deazaadenine[13].