• Archives of Pharmacal Research
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• v.23 no.4
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• pp.288-301
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• 2000

A series of 2-alkyl, 2-aryl, and 2-piperazinyl benzimidazole-4,7-dione derivatives (7a-h) and 16m-o) were prepared, and their cytotoxicities were tested against three cancer cell lines (mouse lymphocytic leukemia cell line P388, and human gastric carcinoma cell lines SNU-1 and SNU-16). These compounds showed potent cytotoxicity against all of three cell lines tested, and especially SNU-16 was sensitive to them. 2-Aryl (7g,h) and 2-piperazinyl benzimidazole-4,7-dione derivative (I6 m) were more potent than mitomycin C against P388 and SNU-16. Among benzimidazole-4,7-dione derivatives with alkyl group at position 2, 7a had the most potent cytotoxicity against all of the cell lines tested.

• Archives of Pharmacal Research
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• v.17 no.6
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• pp.458-461
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• 1994

A new high-performance liquid chromatographic method with column switching has been onto a Bondapak phenyl/corsil $(37-50{\;}{\mu}m)$ precolumn and polar plasma components were washed with 0.06 M borate burffer. After valve switching, the concentrated drug were eluted in the back-flush mode and separated on a ${\mu}-Bondapak$ C18 column with acetonitrilke-phosphate buffer as the mobile phae. The method showed excellent precision, accuracy and speed with detection limit of $0.01{\;}{\mug}/ml^{-1}$. Total analysis time per smaple was less than 20 min and the coefficients of variation for intra and inter-assay were less than 5.635. This method has been successfully applied to plasma smaples from eats after oral administration of omeprazole.

• Archives of Pharmacal Research
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• v.19 no.1
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• pp.62-65
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• 1996

A homologous series of twenty, hitherto unreported, analogues of 5-halosubstituted $1, 3-Bis(\omega-cyanoalkyl)uracil$acyclic nucleosides were synthesized by the series of alkylation reactions of 5-halouracils with the corresponding chloroacetonitrile, chloropropionitrile, chlorobutyronitrile and 5-chlorovaleronitrile $(Cl-(C_ 2)_n-CN: n=l, 2, 3, 4)\; in\; anhydrous\; DMSO\; (or DMF)/K_2CO_3(or NaH)\; under\; 75^{\circ}C$ temperature. Antitumor activities for the synthesized compounds were determined against three cell lines (FM-3A cell, P-388 cell and U-938 cell lines). The compounds that exhibited moderate activity to significant activity, included la-b, 2a-b, 3a-c, and 4a, whose compounds were active against P-388, FM-3A and U-937 cell lines with the compounds la, lb, and 2a, showing significant antitumor activity (inhibitory concentrations $(IC_{50})$ ranged from 2.2 to $7.0\mug/ml$). Their strucrure-activity relationship did not show any activity differences in their effective chain length (methyl, ethyl, propyl, butyl) in 1, 3-bis(.omega.-cyanoalkyl) uracils.

• Journal of the Korean Chemical Society
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• v.47 no.4
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• pp.354-362
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• 2003

A strategy for synthesis of the furan-fused tetracyclic system of xestoquinone was explored through a model study. Using 3-butyn-1-ol as a starting material, 5-iodo-1-methoxymethoxy pentyne (5) was prepared in 5 steps. Reaction of ethyl 2-phenylpropanoate with 5 gave ethyl 7-methoxymethoxy-2-methyl-2-phenyl-5-heptynoate (6) in 88% yield, and then methyl 9-oxo-4-methyl-4-phenyl-2,7-nonadiynoate (13), the key intermediate, was synthesized in 6 steps from the ester 6. Intramolecular cycloaddition reaction of 13 afforded isobenzofuran 14 in 5% yield, which was converted to the tetracyclic structure 15 in the presence of Lewis acid.

• Archives of Pharmacal Research
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• v.19 no.6
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• pp.535-542
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• 1996

Seven isoazamitosene derivatives, mitomycin analogues, were synthesized and tested for cytotoxicities against leukemia and gastric cancer cell lines. Preparation of a pyrrolo[1, 2-a]benzimidazole (3) (azamitosene ring system) was completed by utilizing the Lewis acid-catalized cyclization, with .omicron.-chloronitrotoluene as the starting material. Nitration of 3 produced a mixtue of two isomers (5-nitro isomer (4) and 7-nitro isomer (5)) in product ratio of 36 : 52. 4 was directly converted into quinone (7) by reduction and Fremy oxidaton. Finally, quinone derivatives (8, 9, 10, and 11) were synthesized by 1, 4-addition of 7 with cyclic secondary amines. From above-mentioned 5, 8-nitro compound (15) was prepared in 4 steps. At pH 3, Fremy oxidation of 15 produced quinone (16), whereas iminoquinone derivatives (17a and 17b) at pH 7. Isoazamitosene derivatives (8, 9, 10, and 11), containing cyclic amino groups at the 7-position, showed potent cytotoxicity on P388, SNU-1, and KHH tumor cell lines. Among them, 8 had stronger cytotoxicity against SNU-1 cell line than mitomycin and adriamycin. Considering these results, isoazamitosene derivatives may had unique cytotoxicity profiles. However, isoiminoazamitosene derivatives (17a and 17b) revealed very weak cytotoxicity.

• Archives of Pharmacal Research
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• v.20 no.5
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• pp.410-413
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• 1997

In the course of screening synthetic compounds to inhibit tumor cell growth, pyrrolo[1,2-.alpha.] benzimidazole (PBI), an intermediate of azamitosene, was found to inhibit a proliferation of gastric cancer cell lines. Despite a potential cytotoxic activity against solid tumor cells as opposed to that against rapidly-doubled leukemic cells, there has been no report on the inhibition of gastric cancer cell line by PBI and its' derivatives. The present experiment was designed to determine if PBI derivatives can effectively inhibit the cellular proliferation of gastric cancer cells by using in vitro as well as in vivo chemosensitivity system (MTT assay, clonogenic assay and human tumor xenografted assay). Of the tested PBI derivatives, PBI (18) and PBI (20), displayed the effective growth inhibition of cultured gastric cancer cells or even in the xenografted nude mouse model.

• The Plant Pathology Journal
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• v.22 no.1
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• pp.1-6
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• 2006

The population shifts of Monilinia fructicola isolates which were resistant to the fungicide benzimidazoles were investigated in four regions of Korea from 1998 to 2000. The isolation frequency of benzimidazole-resistant isolates ranged from 18.8% to 29.6% in Chongdo and from $22.0\%$ to $26.8\%$ in Gyeongsan during the same period. However, the frequency of benzimidazoleresistant isolates was less than $4.0\%$ in Chochiwon and Youngduk during the same period. Benzimidazoleresistant isolates showed cross-resistance among benzimidazoles. On the other hand, none of the isolates showed cross-resistance to diethofencarb and carbendazim. Regardless of the year, the benzimidazole-resistant isolates of $EC_{50}$ higher than 500 $\mug%$ a.i./ml were isolated more frequently in mid and late season than in early season. In an orchard of Gyeongsan that had not been exposed to any fungicides for several years, the population of benzimidazole-resistant isolate had persisted without much fluctuation for three years. These results suggest that benzimidazole resistance of M. fructicola is becoming a problem in controlling brown rot and blossom blight of peach in regions like Chongdo and Gyeongsan.

• Journal of Korean Society of Occupational and Environmental Hygiene
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• v.15 no.3
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• pp.176-182
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• 2005

American Conference of Governmental Industrial Hygienists (ACGIH) adopted the Lifting Threshold Limit Values ($TLVs^{(R)}$) in 2005 as a guideline for protecting the workers from work-related low back and shoulder disorders associated with repetitive lifting tasks. The TLVs consist of three tables with recommended weight limits for lifting tasks and their determination procedures are simple. The TLVs sans the material weight/the recommended values (LITLVs) were obtained from 45 lifting tasks in ship engine manufacturing factories. These values were compared and correlated with the Recommended Weight Limits (RWLs) and lifting indices (LIs) determined by the Revised Lifting Equation (LE) of the National Institute for Occupational Safety and Health (NIOSH). The average ratio, LITLVs/LIs, was 0.8 (LITLVs: $1.3{\pm}0.8$, LIs: $1.6{\pm}0.7$). Thus, the TLVs underestimated the risk than the LE. The LITLVs were highly correlated with LIs (r=0.82). The predicted value of LITLVs when LIs=1 wa 0.76. Using the predicted TLVs the higher risk ones of a large number of tasks can be screened to be further investigated.

• International Journal of Industrial Entomology and Biomaterials
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• v.21 no.2
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• pp.163-167
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• 2010

[ $\alpha$ ]Glucosidase (EC 3.2.1.20) is a glycosidase that hydrolyzes disaccharides, oligosaccharides, and polysaccharides resulting in the release of α-D-glucose. In this study, $\alpha$-glucosidase activity in the hemolymph and midgut of the mulberry silkworm Bombyx mori and Japanese oak silkmoth Antheraea yamamai was measured using maltose, sucrose, trehalose, and p-nitrophenyl $\alpha$-D-glucopyranoside as substrates. In general, hemolymph $\alpha$-glucosidase activity was higher in B. mori than in A. yamamai. In contrast, midgut $\alpha$-glucosidase activity was higher in A. yamamai than in B. mori for all of the substrates tested. $\alpha$-Glucosidase activity in the midgut of both B. mori and A. yamamai showed similar responses to changes in pH and temperature for all of the substrates tested. Native (7.5%) PAGE of hemolymph and midgut proteins from B. mori and A. yamamai followed by staining with 4-methylumbelliferyl $\alpha$-D-glucoside (MUG) indicated that the $\alpha$-glucosidases of these related lepidopterans are functionally similar but structurally different. In comparison to $\alpha$-glucosidase activity from A. yamamai, $\alpha$-glucosidase activity from B. mori was generally less sensitive to the $\alpha$-glucosidase inhibitors, 1-deoxynojirimycin (DNJ), acarbose, and voglibose when the activity was determined using maltose, sucrose, and trehalose.

• Journal of the Ergonomics Society of Korea
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• v.27 no.1
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• pp.1-7
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• 2008

Work related musculoskeletal disorders (WMSDs) have become a hot issue within the Korean workplace for the past several years. Recently, the effect of job related stress on WMSDs, cerebro-cardiovascular diseases, and psychiatric disorders has been steadily increasing. The study conducted questionnaire of Korea version job stress model, WMSDs from NIOSH, CES-D (Center for Epidemiologic Studies Depression Scale), and STAI (State-Trait Anxiety Inventory) against train drivers. The results of this study show that the job stress score of the train drivers is high in the areas of physical environment, job latitude, interpersonal conflict, job insecurity, and organization system. The relation between job stress and WMSDs nd, interpersonal conflict, job insecurity and organizational system. The relation between job stress and depressive disorders showed statistical significance in the areas of job demand, job insecurity and low reward. Finally, the relation between job stress and anxiety disorders showed statistical significance in areas of job demand, interpersonal conflict, job insecurity, organizational system and low reward.