• YAKHAK HOEJI
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• v.39 no.6
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• pp.631-635
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• 1995

A series of 3, 4-dihydro-3-oxo-2H-1, 2, 4-benzothiadiazine-1, 1, dioxides with cytotoxic activity against human solid tumors is described. Synthesized compounds showed mild but broad spectrum cytotoxicity in vitro. The lipophilic substituents like alkyl, alkoxy and chloro on benzene ring increased the activity. Also hydrophobic group on 3 or 4 position of benzothiadiazine was important for the activity.

• YAKHAK HOEJI
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• v.40 no.5
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• pp.539-544
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• 1996

4-Aryl-2-hydroxytetronic acids which can be construded as a "lipophilic vitamin C analogue", are known to have antilipidemic and antiaggregatory activities in stead of antiscorb utic activity of vitamin C. A new compound 4-(p-chlorobiphenyl)-2-hydroxytetronic acid (8), which is structurally closely connected with the most active 4-(p-chlorophenyl)-2-hydroxytetronic acid, was synthesized from alpha-(p-chlorobiphenyl)-alpha-hydroxyacetic acid (1) through 7 steps as a potentially bioactive compound.

• YAKHAK HOEJI
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• v.49 no.1
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• pp.60-67
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• 2005

Nonclassical aminobenz[cd]indole antifolates 4, 5 and 6, in which the glutamic acid moiety of the classical antifolates is substituted by 2-phenylglycinamide or 3-aminobenzamide, were synthesized and their in vitro antitumor activity was evaluated. The purpose of this substitution is that the lipophilicity is enhanced due to the aromatic ring of the target compounds for the passive transport through lipid membrane of cells while the hydrogen bonding of the amide is retained in the active site of the enzyme, thymidylate synthase, where the glutamate is originally present. The target compounds were highly cytotoxic against tumor cell lines of murine and human origin with micromolar to nanomolar $IC_{50}$ values. Most effective was compound 4 ($N^6-methyl-N^6$-[4-[(${\alpha}$(S)-aminocarbonylbenzyl) aminocarbonyl]benzyl]-2,6-diaminobenz[cd]indole)with $IC_{50}$ of 2 nM against SW480, human colon adenocarcinoma cell line, which is 650-fold more potent than the reference compound 3.

• YAKHAK HOEJI
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• v.39 no.1
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• pp.61-67
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• 1995

PVC membrane electrodes based on the lipophilic neutral carrier, dibenzo-18-crown-6, cyclic oligomers of teit-butylphenol-formaidehyde condensates, calix[4]arenes as the active sensors for verapamil have been prepared and tested in a variety of plasticizers. At pH 5.0, the electrode exhibits a Nernstian response in the range of 10$^{-2}$~5$\times$10$^{-5}$ M verapamil with a slope of 49.1$\pm$0.5mV per concentration decade. The electrode constructed in this work can be used continuously for at least 1 month before any damage to the membrane occurs. And the analyses of the local anesthetic amine, which are good to select a specific compound in a mixed solution, were also accomplished by using of another neutral carrier, a DB18C6, for comparing with calix[4]arene.

• YAKHAK HOEJI
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• v.47 no.5
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• pp.331-338
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• 2003

A butyrolactone ester of cefazolin (CFZ-BTL) was synthesized by the esterification of cefazolin (CFZ) with $\alpha$-bromo-${\gamma}$-butyrolactone. The synthesis was confirmed by the spectroscopic analysis. The CFZ-BTL was more lipophilic than the CFZ when assessed by n-octanol/water partition coefficients at various pH. The CFZ-BTL itself did not show any antimicrobial activity in vitro, but after oral administration of CFZ-BTL to rabbits, exerted significant anti-microbial activity in serum samples when measured by the inhibion zone method in nutrient agar plates, due to conversion of CFZ-BTL to an active metabolite, probably CFZ, in the body. The CFZ-BTL was also converted into CFZ as confirmed by in vitro incubation study, with tissue homogenates (liver, blood and intestine) of rabbits. The liver showed the fastest conversion rate, probably via the hydrolysis mechanism. In vivo metabolism of CFZ-BTL to CFZ was also confirmed in vivo serum samples by HPLC. The oral bioavailability of CFZ-BTL in rabbits was 1.6-fold increased when compared to CFZ, resulting from followed by enhanced lipophilicity increased passive absorption in the intestine.

• 한국약용작물학회:학술대회논문집
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• 2012.05a
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• pp.189-190
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• 2012

• Journal of the Korean Applied Science and Technology
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• v.15 no.1
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• pp.99-108
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• 1998

Novel type surfactants containing two long-chain hydrophobic alkyl groups and two hydrophilic sulfonate groups were successfully synthesized by reactions of ethylene glycol diglycidyl ether with long-chain fatty alcohols, after then by reactions with 1,3-propane sultone and sodium hydride under THF solvent. All these compounds, so called Gemini surfactants, were purified by thin layer chromatography and column chromatography. Their structures were identified by FT-IR and $^{1}H$-NMR.

• Journal of the Korean Society of Food Science and Nutrition
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• v.20 no.2
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• pp.148-155
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• 1991

Lipid oxidation and browning during fermentation of domestic Meju and Doenjang were examined in order to elucidate the antioxidative effects of browning products and phenol compounds from Meju and Doenjang. Peroxide values of lipids from Meju were detectable and slightly increased until 3 weeks of fermentation, but started to be decreased after 3 weeks of fermentation and notdetectable after 6 weeks. Peroxides were not detected in Doenjang during the whole fermentation, but started to be decreased after 3 weeks of period of 22 weeks fermentation. Carbonyl value were increased during the whole period of Meju fermentation, but started to be decreased at the early stage of Doenjang fermentation. Hydrophilic fraction of browning products from Meju was much higher than lipophilic fraction and the former fraction was dramatically increased at the early stage of the fermentation. But the both fractions maintained high values during Doenjang fermentation. Hydrophilic browning products and phenol and phenol compound in Meju showed strong antioxidative against linoleic acid.

• Bulletin of the Korean Chemical Society
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• v.15 no.10
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• pp.836-841
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• 1994

The polymer matrix effect on the selectivity, response rate and reproducibility for coextraction type anion-selective optode membranes were investigated with DOA-plasticized PVC, PVC/hydroxylated PVC, PU/hydroxylated PVC and DOS-plasticized CTA matrices. Optode membranes were prepared with TDMACl and ETH2412 dissolved in one of the four solvent polymeric matrices. The PU/hydroxylated PVC and PVC-based membranes have almost the same selectivity coefficients, while the CTA-based membrane is more selective toward lipophilic anions. The membrane with PU/hydroxylated PVC adhered strongly to a glass surface, and showed highly reproducible and relatively rapid response. Very poor adhesion of PVC/hydroxylated PVC and CTA-based membranes limited the usability of those membranes as sensor components. Based on these results, and considering the biocompatibility for clinical samples, the optode made with PU/hydroxylated PVC was applied to determine the thiocyanate ion in human saliva. The results obtained with this simple device were comparable to those with rather complicated ISE methods.

• Bulletin of the Korean Chemical Society
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• v.22 no.4
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• pp.405-408
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• 2001

New lipophilic triesters of calix[4]arene and calix[4]quinone are investigated as sodium ion-selective ionophores in poly(vinyl chloride) membrane electrodes. For an ion selective electrode based on calix[4]arene triester I, the linear response is 1 ${\times}$10-3.5 to 1 ${\times}$ 10-1 M of Na+ concentrations. The selectivity coefficients for sodium ion over alkali metal and ammonium ions are determined. The detection limit (logaNa+ = -4.50) and the selectivity coefficient (logKNa+,K+pot = -1.86) are obtained for polymeric membrane electrode containing calix[4]arene triester I.