• Archives of Pharmacal Research
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• v.17 no.6
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• pp.480-482
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• 1994

A number of 5-substituted pyrimidine acyclic nucleosides were synthesized and tested for invitor cytotoxicity against four cell lines (j-82 cell, p-388 cell, FM-3A cell and U-938 cell lines). Synthesis of 1-cyanomethyl-5-substituted pyrimidines (1a-e) and 1-(4-cyanobutyl)-5-substituted pyrimidines (2a-e) was acomplished from the series of alkylation reactions ofl 5-substituted uracils with the corresponding chloacetonitrile and 5-chlorovaleronitile in DMSO under $50^{\circ}C$ temperature. These 5-substituted pyrimidine acylic nucleosides (1a-e and 2a-e) exhibited moderate to significant acitivity aginst four cell lines.

• Analytical Science and Technology
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• v.36 no.4
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• pp.152-160
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• 2023

Adenosine and cordycepin are bioactive compounds with health benefits. Therefore, both substances are often used to assess the quality of Cordyceps products. Optimization and validation of the HPLC/DAD method for determining two nucleosides were studied. The samples were prepared using an ultrasound-assisted extraction (ultrasonic bath). The result was optimal conditions for aqueous extraction, an extraction time of 35 min, and an extraction temperature of 40 ℃. The Chromatographic separation was achieved using a reverse phase column (InfinityLab Poroshell 120 EC-C18, 4.6 × 250 mm, 2.7 ㎛) at 30 ℃ with a mobile phase gradient elution of water and methanol at a flow rate of 0.7 mL/min. The eluents were monitored via a diode array detector at 260 nm. Two nucleosides were separated by less than 12 min after injection. The developed method was found to be excellent linear (r² > 0.9999), accurate (% recovery 95.34-98.51), and precise (% relative standard deviation < 2.0). The limit of detection (LOD) and quantification (LOQ) were 0.45 and 1.38 mg/mL for adenosine and 0.47 and 1.43 mg/mL for cordycepin, respectively. This method was satisfactory for simultaneously quantitating two nucleoside contents, which were used to evaluate Cordyceps products.

• 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.

• Proceedings of the PSK Conference
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• 2001.04a
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• pp.105.3-106
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• 2001

• Bulletin of the Korean Chemical Society
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• v.34 no.3
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• pp.868-874
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• 2013

Efficient synthetic route to novel 2'-spirocyclopropanoid 4'-deoxythreosyl phosphonic acid nucleosides was described from 1,4-dihydroxy-2-butene. Cyclopropane moiety was prepared via ester enolate alkylation using (2-chloroethyl)dimethylsulfonium iodide. Synthesized nucleoside analogues 16, 19, 23 and 26 were tested for anti-HIV activity as well as cytotoxicity. However, none of them showed any anti-HIV activity or cytotoxicity up to 100 ${\mu}M$.

• Archives of Pharmacal Research
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• v.28 no.1
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• pp.16-21
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• 2005

We wanted to elucidate the reason why the trityloxymethyl substituent in $\gamma$-trityloxymethyl-$\gamma$­butyrolactone takes a sterically unfavorable specific conformation, and so we synthesized 5-trityloxymethyldihydrofuran-3-one, 3-(trityloxymethyl)-4-butanolide and 2-trityloxymethyl- tetrahy­drofuran and we then analyzed their conformation by $^{1}H-NMR$ analysis.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1995.10a
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• pp.59-65
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• 1995

후천성 면역결핍증(AIDS)이 전 세계적으로 문제가 된 질병으로 인식된 이래 AIDS의 치료를 위한 새로운 치료제의 개발이 전 세계적으로 중요한 목표가 되어 왔다. 수많은 개발된 물질 중에서 lymphocytes와 macrophage에서의 면역결핍성 바이러스(HIV)에 의한 급성간염을 억제하거나 제거하는데 있어 뉴크레오사이드 유도체들이 아주 중요한 역할을 해오고 있다. 지금까지 개발된 새로운 뉴크레오사이드 유도체중에서 현재 4종류의 뉴크레오사이드 유도체가 FDA에 꼭해 공인이 되어 AIDS환자의 치료에 사용되고 있다.

• Archives of Pharmacal Research
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• v.26 no.12
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• pp.990-996
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• 2003

A novel carboacyclic nucleoside analogue, 9-[2-bromo-4-hydroxy-3-hydroxymethyl-2-butenyl] adenine, and its derivatives were designed and synthesized as open-chain analogues of neplanocin A. The syntheses were accomplished via the coupling of adenine or pyrimidine bases to the key intermediate allylic bromide 7. The bromide 7 was prepared from epichlorohydrin in a seven step process in a 54% overall yield. The synthesized compounds were evaluated for their antiviral activity against the polio virus, HSV and HIV.

• Bulletin of the Korean Chemical Society
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• v.25 no.11
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• pp.1714-1716
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• 2004

• YAKHAK HOEJI
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• v.33 no.5
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• pp.296-299
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• 1989

The synthetic study of 2', 3'-diazido and difluoro secouridines toward development of new antiviral agents is discribed. These acyclic nucleosides were synthesized from uridine by the method of ring opening reaction of sugar moiety.