• Archives of Pharmacal Research
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• v.18 no.5
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• pp.364-365
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• 1995

• Archives of Pharmacal Research
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• v.19 no.3
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• pp.243-245
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• 1996

• YAKHAK HOEJI
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• v.32 no.3
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• pp.177-181
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• 1988

Methyl 6-0-benzoyl-3-0-benzyl-2, 5-di-deoxy-2-fluoro-allofuranose (11) and 1, 2-0-di-acetyl-6-0-benzoyl-3, 5-di-deoxy-3-fluoro-glucofuranoes (22), sugar moieties of potential antiviral and/or anticancer chemotherapeutic nucleoside, were synthesized from D-glucose.

• Archives of Pharmacal Research
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• v.6 no.1
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• pp.79-81
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• 1983

Several potent anti-herpes virus nucleosides, 2'fluoro-2'-deoxyarabinofuranosyl pyrimidine nucleosides, were prepared in good yields by a new condensation method using sodium iodide and a new solvent system, and FMAU could be also prepared directly from thymine by this method.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.223-223
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• 1994

FDA가 공인한 항 HIV제로서 사용중인 AZT나 DDI와 같은 화합물은 장기 투여로 심각한 부작용들이 나타나고 있다. 그래서 기존의 activity를 가진 nucleoside류의 sugar 부분에 새로운 base 즉, 5-ethoxymethyl uracil을 축합, 3'-azido-2',3'-dideoxy-5-ethoxy-methyl uridine, 2',3'-aideoxy-3'-fluoro-5-ethoxymethyl uridine과 2',3'-dideoxy-5-ethoxymethyl uridine들을 합성, 구조활성 상관관계를 검토하였다. 이들의 합성은 먼저 적절한 group으로 sugar의 -OH group을 보호한후 uracil류와 반응, uridine 유도체를 먼저 합성하였다. 각각의 uridine 유도체들의 5-위치에 ethoxymethyl group을 도입하기 위해 formalin과 반응시킨후 5-hydroxy-methyl group을 도입하고 산촉매 하에 ethanol과 반응, ethyl ether류를 합성하였다.

• Archives of Pharmacal Research
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• v.12 no.4
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• pp.300-305
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• 1989

The synthetic study of 3' azido and 3'-fluoro secouridines toward development of new antiviral agents is described. These acyclic nucleosides were synthesized from uridine by the method of ring opening reaction of sugar moiety.

• YAKHAK HOEJI
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• v.40 no.2
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• pp.117-125
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• 1996

3'-Deamino-3-hydroxy-4'-fluoro- or 3'-deamino-3'-hydroxy-4'-azido-daunorubicin(6,8) and -doxorubicin(7,9) have been synthesized, respectively. Compounds 7,8 and 9 were mo re cytotoxic than daunorubicin(1) and doxorubicin(2) against L1210 murine leukemic cell in vitro. When administered intraperitoneally for 9 days starting 1 day after tumor inoculation, compounds 7(T/C 605%) and 9(T/C 488%) showed significant antitumor activity for ip-inoculuated L1210 murine leukemia at wide range of doses.

• Journal of The Korean Society of Inherited Metabolic disease
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• v.13 no.2
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• pp.89-97
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• 2013

Purpose: We retrospectively investigated individuals who hadbeen identified by neonatal screening as potential galactosemia patients to determine the etiology of galactosemia. Methods: One hundred fifty-three patients referred to Korea Genetics Research Center due to high galactose level detected by neonatal screening test between February 2005 and May 2013 were examined. Galactose and galactose-1-phosphate levels were measured by using a fluoro metric microplate reader. Lactose free diet was initiated immediately after confirmed by urine Clinitest. If reducing sugar was negative, we employed abdominal sonogram and echocardiogram to check for possible porto-systemic shunt. Results: Fifteen patients were diagnosed with galactosemia. One patient had galactokinase (GALK) deficiency; four had UDP galactose-4-epimerase (GALE) deficiency; two had citrin deficiency; and four had porto-systemic shunt. Two had unknown causes of galactosemia. Conclusion: In addition to genetic defects of GALT, GALK and GALE, citrin deficiency or porto-systemic shunt could also cause galactosemia. It is crucial to carry out differential diagnosis to determine the cause of galactosemia.

• Bulletin of the Korean Chemical Society
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• v.28 no.12
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• pp.2449-2453
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• 2007

L-[18F]FMAU ([18F]1b) was prepared from the precursor 2-O-[(trifluoromethyl)-sulfonyl]-1,3,5-tri-Obenzoyl- α-L-ribofuranose, by coupling the radioactive fluoro-sugar with the corresponding silylated thymine in 4 steps. The final products, including the α and β anomers, were purified using reverse phase HPLC with an appropriate solvent (5% CH3CN/H2O) at a flow rate of 3.0 mL/min. The total elapsed time of synthesis was about 180-200 min from EOB. The α/β anomeric ratio of the compounds was about 1:9, and the radiochemical purity of the product (β-form) was >98% with decay-corrected yields of 25-35%. All radioactive samples were confirmed using co-injection with pure non-radioactive analogues in every step. In the cellular uptake in vitro test of herpes simplex virus-thymidine kinase (HSV1-TK) gene expressed cells, the percent uptake of injected dose (%ID) of L- and D-FMAU was 37.28 and 65.86, respectively after 240 min incubation. However, the relative uptake (MCA-TK/MCA cellular uptake ratio) of L-FMAU was higher than that of D-FMAU (%ID of L-FMAU, 0.36 and D-FMAU, 0.93 after 240 min incubation in MCA cells). This means that L-FMAU will show better specific HSV1-TK gene expressed cell uptake for selective HSV1-TK gene imaging.