Research Topics
Genomes and GenesSpecies | Lak Shin JeongSummaryAffiliation: Ewha Womans University Country: Korea Publications
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Publications
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonistsLak Shin Jeong
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Korea
J Med Chem 50:3159-62. 2007..An N6-(3-chlorobenzyl)purine analogue 9b displayed a Ki value of 1.66 nM at the human A3 AR. Thus, truncated D-4'-thioadenosine is an excellent template for the design of novel A3 AR antagonists to act at both human and murine species...- Stereoselective synthesis of 1'-functionalized-4'-thionucleosidesLak Shin Jeong
College of Pharmacy, Ewha Womans University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 26:1011-4. 2007..Stereoselective functionalization of the 1'-position of 4'-thionucleosides was achieved using a stereoselective S(N)2 reaction controlled by 5-membered ring coordination... 
Design and synthesis of novel 2',3'-dideoxy-4'-selenonucleosides as potential antiviral agentsLak Shin Jeong
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Republic of Korea
Bioorg Med Chem 16:9891-7. 2008....- Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptorLak Shin Jeong
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, South Korea
Bioorg Med Chem Lett 14:4851-4. 2004.... - Recent advances in the synthesis of the carbocyclic nucleosides as potential antiviral agentsLak Shin Jeong
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul, South Korea
Antivir Chem Chemother 15:235-50. 2004..Furthermore, the review includes valuable information for designing and synthesizing novel carbocyclic nucleosides... - Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonistsLak Shin Jeong
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Korea
J Med Chem 51:6609-13. 2008..5 nM), but a N(6)-(3-bromobenzyl) derivative 7d showed the optimal species-independent binding affinity... - Synthesis of N6-substituted 3'-ureidoadenosine derivatives as highly potent agonists at the mutant A3 adenosine receptorLak Shin Jeong
College of Pharmacy, Ewha Womans University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 26:717-9. 2007..Among compounds tested, 3 '-ureido-N6-(3-iodobenzyl)adenosine (2c) exhibited the highest binding affinity (Ki = 0.22 micro M) at the H272E mutant A3 AR without binding to the natural A3AR... - Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptorLak Shin Jeong
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Korea
J Med Chem 49:273-81. 2006..In several cases for which the corresponding 4'-oxonucleosides have been studied, the 4'-thionucleosides showed higher binding affinity to the A(3) AR... - Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonistsLak Shin Jeong
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Republic of Korea
Bioorg Med Chem Lett 18:1612-6. 2008..A N(6)-(3-bromobenzyl) derivative 6c (K(i)=9.32 nM) exhibited the highest binding affinity at the human A(3)AR with very low binding affinities to other AR subtypes... - Design, synthesis, and biological activity of N6-substituted-4'-thioadenosines at the human A3 adenosine receptorLak Shin Jeong
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Republic of Korea
Bioorg Med Chem 14:4718-30. 2006..N6-(3-Iodobenzyl) derivative 19g was demonstrated to be an A3AR-selective partial agonist displaying a Ki value of 3.2 nM... - First synthesis of 4'-selenonucleosides showing unusual Southern conformationLak Shin Jeong
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Korea
Org Lett 10:209-12. 2008..All stereoelectronic effects shown in 4'-oxonucleosides were overwhelmed by the size of selenium and steric interactions, driving the conformation to the C2'-endo/ C3'-exo twist (Southern) conformation... - Synthesis and anti-HCV activity Of 2''-beta-hydroxymethylated nucleosidesLak Shin Jeong
College of Pharmacy, Ewha Womans University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 26:725-8. 2007..Adenine nucleoside 3 showed potent anti-HCV activity, implying that 2' -beta-hydroxymethyl group has the appropriate electronic properties interfering with HCV polymerase... - Asymmetric synthesis of novel apio carbocyclic nucleoside analogues as potential antiviral and antitumor agentLak Shin Jeong
College of Pharmacy, Ewha Womans University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 26:721-4. 2007..Novel apio carbocyclic nucleosides 18-21 were asymmetrically synthesized as potential antiviral and antitumor agent, starting from D-ribose employing aldol reaction, RCM reaction and Mitsunobu reaction as key reactions... - Synthesis and antitumor activity of fluorocyclopentenyl-pyrimidinesLak Shin Jeong
College of Pharmacy, Ewha Womans University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 26:713-6. 2007..Cytosine analog 8 was found to exhibit significant anticancer activity in various human tumor cell lines... - Design, synthesis, and anti-tumor activity of 4'-thionucleosides as potent and selective agonists at the human A3 adenosine receptorLak Shin Jeong
College of Pharmacy, Ewha Womans University, Seoul 120 750, Korea
Nucleosides Nucleotides Nucleic Acids 26:1565-8. 2007..38 nM and 0.28 nM, respectively) at the human A(3)AR. These compounds showed anti-growth effects on HL-60 leukemia cell, which resulted from the inhibition of Wnt signaling pathway... - Asymmetric synthesis of cyclopropyl-fused 2'-C-methylcarbanucleosides as potential anti-HCV agentsLak Shin Jeong
College of Pharmacy, Ewha Womans University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 26:1021-4. 2007..Novel 2'-C-methyl-cyclopropyl-fused carbocyclic nucleosides as potential anti-HCV agents were stereoselectively synthesized, utilizing regioselective cleavage of the isopropylidene group and cyclic sulfate chemistry as key steps... - Discovery of a new template for anticancer agents: 2'-deoxy-2'-fluoro-4'-selenoarabinofuranosyl-cytosine (2'-F-4'-seleno-ara-C)Lak Shin Jeong
Department of Bioinspired Science, Division of Life and Pharmaceutical Sciences, College of Pharmacy, Ewha Womans University, Seoul, Korea
J Med Chem 52:5303-6. 2009..Among compounds tested, 2'-F-4'-seleno-ara-C (4a) exhibited highly potent anticancer activity in all cancer cell lines tested and was more potent than ara-C (1)... - Synthesis of halogenated 9-(dihydroxycyclopent-4'-enyl) adenines and their inhibitory activities against S-adenosylhomocysteine hydrolaseLak Shin Jeong
College of Pharmacy, Ewha Womans University, Seoul, South Korea
Nucleosides Nucleotides Nucleic Acids 22:919-21. 2003..Novel halovinyl analogues of neplanocin A without 4'-hydroxymethyl group were easily synthesized starting from D-ribose via cyclopentenone 5 as a key intermediate and their inhibitory activity against SAH hydrolase was assayed... - Synthesis and biological evaluation of halo-neplanocin A as novel mechanism-based inhibitors of S-adenosylhomocysteine hydrolaseLak Shin Jeong
College of Pharmacy, Ewha Womans University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 22:589-92. 2003..Halogenated analogues of neplanocin A were synthesized from the key intermediate 1, among which fluoro-neplanocin A was found to be novel mechanism-based irreversible inhibitor of S-Adenosylhomocysteine hydrolase... - N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptorLak Shin Jeong
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Korea
J Med Chem 46:3775-7. 2003..28 +/- 0.09 nM). 4 was also selective for A(3) vs human A(1) and human A(2A) receptors by 4800- and 36000-fold, respectively... - Design, synthesis, and biological evaluation of fluoroneplanocin A as the novel mechanism-based inhibitor of S-adenosylhomocysteine hydrolaseLak Shin Jeong
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Korea
J Med Chem 46:201-3. 2003..A new mechanism of irreversible inhibition discovered in this work might provide new alternatives in the design of a different class of antiviral agents operating via SAH inhibition... - Synthesis of 3'-ureidoadenosine analogues and their binding affinity to the A3 adenosine receptorMoon Woo Chun
Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 24:1119-21. 2005..However, all synthesized 3'-ureidoadenosine analogues have lost their binding affinities to the all subtypes of adenosine receptors, indicating that bulky 3'-urea moiety led to conformational distortion... - Design, synthesis and binding affinity of 3'-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligandsMoo Hong Lim
College of Pharmacy, Seoul National University, Seoul 151-742, South Korea
Bioorg Med Chem Lett 13:817-20. 2003.... 
Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonistsWon Jun Choi
Department of Bioinspired Science and Division of Life and Pharmaceutical Sciences, College of Pharmacy, Ewha Womans University, Seoul 120 750, Republic of Korea
Bioorg Med Chem 17:8003-11. 2009..4 nM). Bulky substituents at the 5'-uronamide position, such as cyclohexyl and 2-methylbenzyl, in this series of 2-H nucleoside derivatives were tolerated in A(3)AR binding, although small alkyl analogues were more potent...- Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonistsShantanu Pal
Department of Bioinspired Science and Division of Life and Pharmaceutical Sciences, Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Republic of Korea
Bioorg Med Chem 17:3733-8. 2009..Although the 4'-oxo series were less potent than the 4'-thio series, this class of human A(3) AR antagonists is also regarded as another good template for the design of A(3) AR antagonists and for further drug development... - Stereoselective synthesis of conformationally rigid apio carbanucleosides as potential antiviral agentsHyung Ryong Moon
College of Pharmacy, Pusan National University, Pusan 609-735, Korea
Nucleosides Nucleotides Nucleic Acids 24:709-11. 2005..Introduction of hydroxymethyl substituent was efficiently and stereoselectively accomplished by aldol and retro-aldol reaction and fixed conformation was achieved from a modified Simmons-Smith cyclopropanation on a cyclopentane ring... - Design, synthesis, and molecular modeling studies of 5'-deoxy-5'-ureidoadenosine: 5'-ureido group as multiple hydrogen bonding donor in the active site of S-adenosylhomocysteine hydrolaseTing Wang
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Republic of Korea
Bioorg Med Chem Lett 17:4456-9. 2007.... - Structure-activity relationship of 5'-substituted fluoro-neplanocin a analogues as potent inhibitors of S-adenosylhomocysteine hydrolaseHyung Ryong Moon
College of Pharmacy, Pusan National University, Pusan 609-735, Korea
Nucleosides Nucleotides Nucleic Acids 24:707-8. 2005.... - Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A₂A and A₃ adenosine receptor ligandsXiyan Hou
Laboratory of Medicinal Chemistry, College of Pharmacy, and Department of Bioinspired Science, Ewha Womans University, Seoul 120 750, Korea
J Med Chem 55:342-56. 2012..Compound 4g was the most potent ligand acting dually as hA(2A)AR agonist and hA(3)AR antagonist, which might be useful for treatment of asthma or other inflammatory diseases... - Stereoselective synthesis and conformational study of novel 2',3'-Didehydro-2',3'-dideoxy-4'-selenonucleosidesDilip K Tosh
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul, Korea
J Org Chem 73:4259-62. 2008..Introduction of 2',3'-double bond was achieved by treating cyclic 2',3'-thiocarbonate with 1,3-dimethyl-2-phenyl-1,3,2-diazaphospholidine... - Design and synthesis of A3 adenosine receptor ligands, 3'-fluoro analogues of Cl-IB-MECAHea Ok Kim
Division of Chemistry and Molecular Engineering, Seoul National University, Seoul, South Korea
Nucleosides Nucleotides Nucleic Acids 22:923-5. 2003..Synthesis of 3'-deoxy-3'-fluoro-N6-substituted adenosines as bioisosteres of Cl-IB-MECA and their binding affinities to A3 adenosine receptor are described... - Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activityWon Jun Choi
Department of Bioinspired Science and College of Pharmacy, Ewha Womans University, Seoul 120 750, Korea
J Med Chem 55:4521-5. 2012..However, its 2'-deoxycytidine derivative 5b did not show any antigrowth effects, indicating that 2'-hydroxyl group is essential for the biological activity... - Design, synthesis, and biological evaluation of novel iso-D-2',3'-dideoxy-3'-fluorothianucleoside derivativesKyung Ran Kim
Laboratory of Medicinal Chemistry, College of Pharmacy and Research Institute for Drug Development, Pusan National University, Busan 609 735, Republic of Korea
Bioorg Med Chem 15:227-34. 2007..43microg/mL). This result implies that iso-2',3'-dideoxy sugar templates might play a role of a sugar surrogate of nucleosides for the development of anti-RNA virus agent... - Synthesis of novel apio carbocyclic nucleoside analogues as selective a(3) adenosine receptor agonistsJeong A Lee
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea
J Org Chem 70:5006-13. 2005.... - Stereoselective synthesis of homo-apioneplanocin A as potential inhibitor of S-adenosylhomocysteine hydrolaseMoon Woo Chun
College of Pharmacy, Seoul National University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 26:729-32. 2007.... - Stereoselective synthesis of novel thioiso dideoxy nucleosides with exocyclic methylene as potential antiviral agentsPrashantha Gunaga
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 24:1115-7. 2005..Cyclization of the dimesylate to the 4-thiosugar 6a proceeded in pure SN2 reaction in the presence of allylic functional group... - Design, synthesis, and in vitro evaluation of APIO analogue of neplanocin AHyung Ryong Moon
College of Pharmacy, Ewha Womans University, Seoul, South Korea
Nucleosides Nucleotides Nucleic Acids 22:1475-7. 2003.... - Synthesis of 5'-substituted fluoro-neplanocin A analogues: importance of a hydrogen bonding donor at 5'-position for the inhibitory activity of S-adenosylhomocysteine hydrolaseHyung Ryong Moon
College of Pharmacy, Pusan National University, Pusan 609-753, Korea
Bioorg Med Chem Lett 14:5641-4. 2004..All the final compounds showed much less decreased cytotoxicity in two cancer cell lines (Col2 and A549), implying that phosphorylation of the 5'-hydroxyl group of fluoro-neplanocin A is closely related to its high cytotoxicity... - Design and synthesis of A3 adenosine receptor ligands, 2'-fluoro analogues of Cl-IB-MECAHea Ok Kim
Division of Chemistry and Molecular Engineering, Seoul National University, Seoul, South Korea
Nucleosides Nucleotides Nucleic Acids 22:927-30. 2003..Synthesis of 2'-deoxy-2'-fluoro-N6-substituted adenosines as bioisosteres of Cl-IB-MECA and their binding affinities to A3 adenosine receptor are described... - Stereoselective synthesis of 3-hydroxymethyl-D-cyclopentenone, the versatile intermediate for the synthesis of carbocyclic nucleosidesWon Jun Choi
WonJun Choi Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea
Nucleosides Nucleotides Nucleic Acids 24:611-3. 2005..The preparative and stereoselective synthesis (45- 50% overall yields, >50 g scale) of the key carbasugars 7a-d was achieved from D-ribose via stereoselective Grignard reaction and oxidative rearrangement as key reactions... - A new DNA building block, 4'-selenothymidine: synthesis and modification to 4'-seleno-AZT as a potential anti-HIV agentVarughese Alexander
Department of Bioinspired Science and Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Korea
Org Lett 12:2242-5. 2010..4'-Selenothymidine (1) was discovered to adopt the same 2'-endo/3'-exo conformation as thymidine, which is unusual in that 4'-selenouridine has the opposite conformation to that of uridine... - Design, synthesis, and binding of homologated truncated 4'-thioadenosine derivatives at the human A3 adenosine receptorsHyuk Woo Lee
Department of Bioinspired Science, College of Pharmacy, Ewha Womans University, Seoul 120 750, Republic of Korea
Bioorg Med Chem 18:7015-21. 2010.... - Synthesis of 2-alkynyl substituted 4'-thioadenosine derivatives and their binding affinities at the adenosine receptorsCheng Wu Liang
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Korea
Arch Pharm Res 31:973-7. 2008..Among compounds tested, only compound 3b showed moderate binding affinity at the human A3 adenosine receptor without binding affinities at other subtypes... - X-ray crystal structure and binding mode analysis of human S-adenosylhomocysteine hydrolase complexed with novel mechanism-based inhibitors, haloneplanocin A analoguesKang Man Lee
College of Pharmacy, Ewha Womans University, Seoul 120 750, Korea
J Med Chem 54:930-8. 2011..The inhibitory activity was decreased as the size of the halogen atom increased and/or if the 4'-CH(2)OH group was absent. These results could be utilized to design new therapeutic agents operating via AdoHcy hydrolase inhibition... - Synthesis of 5-azacytidine nucleosides with rigid sugar moiety as potential antitumor agentsMoon Woo Chun
College of Pharmacy, Seoul National University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 22:915-7. 2003..The bicyclic 3'-O,5'-C-methylene-linked and 2'-O,5'-C-methylene-linked 5-azacytidine derivatives were readily synthesized from 1,2;5,6-di-O-isopropylidene-D-glucose and evaluated against several cancer cell lines... - Synthesis of [1'-fluoro-2',2'-bis-(hydroxymethyl)cyclopropylmethyl]purines as antiviral agentsJu-Hyun Park
College of Pharmacy, Sookmyung Women's University, Yongsangu, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 22:955-7. 2003..1'-Fluoro-2',2'-bis-(hydroxymethyl)cyclopropylmethyl]purines were designed, synthesized and their antiviral activity against poliovirus, HSV and HIV was evaluated... - Synthesis of 3'-deoxy-3'-C-hydroxymethyl analogues of tiazofurin and ribavirinMoon Woo Chun
Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Korea
Nucleosides Nucleotides Nucleic Acids 24:975-7. 2005..On the basis of potent biological activity of 3'-branched-3'-deoxynucleoside analogues, novel ribavirin and tiazofurin derivatives with 3'-C-hydroxymethyl substituent were synthesized, starting from D-xylose... - Synthesis of D- and L-apio nucleoside analogues with 2'-hydroxyl group as potential anti-HIV agentsDong Zhe Jin
College of Pharmacy, Seoul National University, Seoul 151-742, South Korea
Bioorg Med Chem 12:1101-9. 2004.... - Synthesis of 3'-acetamidoadenosine derivatives as potential A3 adenosine receptor agonistsMoon Woo Chun
College of Pharmacy, Seoul National University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 27:408-20. 2008.... - Preparative and stereoselective synthesis of the versatile intermediate for carbocyclic nucleosides: effects of the bulky protecting groups to enforce facial selectivityWon Jun Choi
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea
J Org Chem 69:2634-6. 2004.... - Synthesis of 3'-C-hydroxymethyl-substituted pyrimidine and purine nucleosides as potential anti-hepatitis C virus (HCV) agentsXiaojuan Pei
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul, Korea
Arch Pharm Res 31:843-9. 2008.... - Regio- and stereoselective synthesis of truncated 3'-aminocarbanucleosides and their binding affinity at the A3 adenosine receptorMun Ju Choi
Laboratory of Medicinal Chemistry, College of Pharmacy and Department of Bioinspired Science, Ewha Womans University, Seoul, 120 750, Korea
Org Biomol Chem 9:6955-62. 2011..The stereoselective synthesis of truncated 3'-aminocarbanucleosides 4a-d via a stereo- and regioselective conversion of a diol 9 to bromoacetate 11a and their binding affinity towards the human A(3) adenosine receptor are described... - Synthesis and biological evaluation of novel tert-azido or tert-amino substituted penciclovir analogsHea Ok Kim
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea
Org Biomol Chem 2:1164-8. 2004.... - Stereoselective synthesis of a novel apio analogue of neplanocin A as potential S-adenosylhomocysteine hydrolase inhibitorHyung Ryong Moon
College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea
Org Lett 4:3501-3. 2002..reaction: see text].. - Synthesis of homo-N-nucleoside with 1,2,4-triazole-3-carboxamideMoon Woo Chun
Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Korea
Nucleosides Nucleotides Nucleic Acids 24:979-81. 2005.... - Synthesis of fluorinated cyclopentenyladenine as potent inhibitor of S-adenosylhomocysteine hydrolaseHea Ok Kim
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120-750, South Korea
Bioorg Med Chem Lett 14:2091-3. 2004..From this study, 4(')-hydroxymethyl groups of neplanocin A and fluoro-neplanocin A played an important role in binding to the active site of the enzyme... - Synthesis and biological evaluation of novel thioapio dideoxynucleosidesHyung Ryong Moon
College of Pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea
Bioorg Med Chem 10:1499-507. 2002..Although we could not find good anti-HIV agents in this study, findings of some anticancer activity in this series will allow this class of nucleosides to be the new template for the development of new anticancer agents (Fig. 1)... - Stereoselective synthesis of 2'-C-methyl-cyclopropyl-fused carbanucleosides as potential anti-HCV agentsJeong A Lee
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea
Org Lett 8:5081-3. 2006..reaction: see text].. - Asymmetric synthesis of novel thioiso dideoxynucleosides with exocyclic methylene as potential antiviral agentsPrashantha Gunaga
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea
J Org Chem 69:3208-11. 2004..On the other hand, glycosylation of 14 with 6-chloropurine under Mitsunobu conditions afforded the desired S(N)2 product 26, while palladium-catalyzed glycosylation resulted in the sole formation of S(N)2' product 34... - Synthesis of 2-C-hydroxymethylribofuranosylpurines as potent anti-hepatitis C virus (HCV) agentsByul Nae Yoo
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul, Republic of Korea
Bioorg Med Chem Lett 16:4190-4. 2006..Among compounds tested, adenosine derivative 2a exhibited potent anti-HCV activity, indicating that the hydroxyl group of 2'-C-hydroxymethyl substituent led to favorable interaction with HCV polymerase... - Synthesis and anti-hepatitis C virus (HCV) activity of 3'-C-substituted-methyl pyrimidine and purine nucleosidesWon Jun Choi
Department of Bioinspired Science, Ewha Womans University, 11 1 Seodaemun gu, Daehyun dong, Seoul 120 750, Republic of Korea
Bioorg Med Chem 18:4812-20. 2010..This study guarantees the 3'-C-substituted-methyl nucleoside serves as a new template for the development of new anti-HCV agents... - Synthesis of novel L-N-MCd4T as a potent anti-HIV agentAh-Young Park
Laboratory of Medicinal Chemistry, College of Pharmacy and Research Institute for Drug Development, Pusan National University, Busan, Korea
Org Biomol Chem 4:4065-7. 2006..76 microg mL(-1)) agent without cytotoxicity up to 100 microg mL(-1), indicating that the anti-HIV-1 activity found is similar to that of ddI (EC50 = 4.95 microg mL(-1)), which is used clinically for the treatment of AIDS patients... - Synthesis and biological evaluation of pyrimidine nucleosides fused with 3',4'-tetrahydrofuran ringMoon Woo Chun
College of Pharmacy, Seoul National University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 22:719-21. 2003..Thymine analogue 1 and its corresponding 2'-deoxy analogue 3 exhibited high cytotoxicity instead of giving antiviral activities... - Alternative and improved syntheses of highly potent and selective A3 adenosine receptor agonists, Cl-IB-MECA and thio-Cl-IB-MECAXiyan Hou
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120 750, Korea
Arch Pharm Res 30:1205-9. 2007..New synthetic methods were found to be superior to old methods from the viewpoint of use of cheap starting material, number of steps, and overall yields... - Synthesis of (Z)-(1-fluoro-2-hydroxymethylcyclopropylmethyl)purinesJu-Hyun Park
College of Pharmacy, Sookmyung Women's University, Yongsangu, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 22:659-61. 2003..Z)-(1-fluoro-2-hydroxymethylcyclopropylmethyl)purines were designed, synthesized and evaluated their antiviral activity against poliovirus, HSV, and HIV... - Inhibition of cell proliferation through cell cycle arrest and apoptosis by thio-Cl-IB-MECA, a novel A3 adenosine receptor agonist, in human lung cancer cellsSun Jack Kim
College of Pharmacy, Ewha Womans University, 11 1 Daehyun Dong, Seodaemun Ku, Seoul 120 750, Republic of Korea
Cancer Lett 264:309-15. 2008..The activation of Akt-mediated signaling was also inhibited by treatment with thio-Cl-IB-MECA. These data might suggest the potential therapeutic value of an adenosine analog in the treatment of human lung cancer... - Synthesis of fluoroneplanocin ALak Shin Jeong
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul, Korea
Curr Protoc Nucleic Acid Chem . 2008..This intermediate is synthesized using a stereoselective Grignard reaction, a ring-closing metathesis (RCM) reaction, and oxidative rearrangement as key steps... - Synthesis of 2-(3'-azido- and 3'-amino-3'-deoxy-beta-D-ribofuranosyl)thiazole-4-carboxamideCheng Wu Liang
College of Pharmacy, Seoul National University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 22:2039-48. 2003..In view of biological activities of tiazofurin and azido or aminosugar nucleosides, novel azido- and amino-substituted tiazofurin derivatives (1 and 2) were efficiently synthesized starting from 1,2;5,6-di-O-isopropylidene-D-glucose... - A novel adenosine analog, thio-Cl-IB-MECA, induces G0/G1 cell cycle arrest and apoptosis in human promyelocytic leukemia HL-60 cellsEun-Jin Lee
College of Pharmacy, Ewha Womans University, 11-1 Daehyun-dong, Seodaemun-ku, Seoul 120 750, Republic of Korea
Biochem Pharmacol 70:918-24. 2005.... - Recent advances in 4'-thionucleosides as potential antiviral and antitumor agentsPrashantha Gunaga
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul, 120-750, Korea
Curr Med Chem 11:2585-637. 2004..and Walker et al. Subsequent contributions by the other authors, enhanced its standing as an important class of antiviral agents. Following is a reasonably exhaustive account of this class of compounds reported after 1990... - Truncated fluorocyclopentenyl pyrimidines as S-adenosylhomocysteine hydrolase inhibitorsYeon Hee Park
Department of Bioinspired Science and Division of Life and Pharmaceutical Sciences, College of Pharmacy, Ewha Womans University, Seoul, Korea
Nucleosides Nucleotides Nucleic Acids 28:601-13. 2009.... - Structural determinants of efficacy at A3 adenosine receptors: modification of the ribose moietyZhan-Guo Gao
Laboratory of Bioorganic Chemistry, Molecular Recognition Section, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
Biochem Pharmacol 67:893-901. 2004.... - Synthesis of enantiopure pseudo-L-vinylcyclopropyl nucleosides bearing quaternary carbon as potential anti-herpesvirus agentHyung Ryong Moon
College of Pharmacy and Research Institute for Drug Development, Pusan National University, Busan, Korea
Nucleosides Nucleotides Nucleic Acids 26:975-8. 2007.... - D-4'-thioadenosine derivatives as highly potent and selective agonists at the human A3 adenosine receptorHyouk Woo Lee
College of Pharmacy, Seoul National University, Seoul [corrected] Korea
Nucleosides Nucleotides Nucleic Acids 24:607-9. 2005..28 +/- 0.09 nM) at the human A3 adenosine receptor... - Asymmetric synthesis of novel pseudo-D-vinylcyclopropyl nucleosides bearing quaternary carbon as potential anti-herpesvirus agentAh Young Park
College of Pharmacy and Research Institute for Drug Development, Pusan National University, Busan, Korea
Nucleosides Nucleotides Nucleic Acids 26:1001-4. 2007.... - Asymmetric synthesis of apio fluoroneplanocin A analogs as potential AdoHcy hydrolase inhibitorAh Young Park
College of Pharmacy and Research Institute for Drug Development, Pusan National University, Busan, Korea
Nucleosides Nucleotides Nucleic Acids 26:943-7. 2007..This methodology can be adapted to the synthesis of fluoro compounds extensively... - Design, enantiopure synthesis, and biological evaluation of novel iso-D-2',3'-dideoxy-3'-fluorothianucleoside derivatives as a bioisostere of lamivudineKyung Ran Kim
College of Pharmacy and Research Institute for Drug Development, Pusan National University, Busan, Korea
Nucleosides Nucleotides Nucleic Acids 26:911-5. 2007..43 microg/mL). This result implies that iso 2',3'-dideoxy sugar templates might play a role of a sugar surrogate of nucleosides for the development of anti-RNA virus agent... - Probing the binding site of the A1 adenosine receptor reengineered for orthogonal recognition by tailored nucleosidesKrishnan K Palaniappan
Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892 0810, USA
Biochemistry 46:7437-48. 2007..This neoceptor approach should be useful for the validation of molecular modeling and the dissection of promiscuous GPCR signaling... - Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptorSoo-Kyung Kim
Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK, National Institutes of Health (NIH, Bethesda, MD 20892, USA
J Mol Graph Model 25:562-77. 2006..Thus, the putative conformational changes associated with A(3)AR activation indicate a shared mechanism of GPCR activation similar to rhodopsin... - Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonistsZhan-Guo Gao
Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA
J Med Chem 49:2689-702. 2006..The orthogonal pair comprising an engineered receptor and a modified agonist should be useful for elucidating signaling pathways and could be therapeutically applied to diseases following organ-targeted delivery of the neoceptor gene... - The antitumor effect of LJ-529, a novel agonist to A3 adenosine receptor, in both estrogen receptor-positive and estrogen receptor-negative human breast cancersHeekyoung Chung
Department of Pathology, College of Medicine, Hanyang University, 133-791 Seoul, Republic of Korea
Mol Cancer Ther 5:685-92. 2006.... - Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5'-ribofuran-uronamide moietyZhan-Guo Gao
Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA
Bioorg Med Chem Lett 16:596-601. 2006..Competitive antagonism was demonstrated by Schild analysis. The 2-(dimethylamino)-5'-(N,N-dimethyl)uronamido substitution also retained A(3)AR selectivity but lowered affinity... - Synthesis and biological evaluation of novel D-2'-azido-2',3'-dideoxyarabinofuranosyl-4'-thiopyrimidines and purinesHea Ok Kim
Division of Chemistry and Molecular Engineering, Seoul National University, Seoul 151-742, Republic of Korea
Bioorg Med Chem Lett 12:2403-6. 2002..Most of the final nucleosides exhibited toxicity-dependent anti-HIV-1 activity, among which D-alpha-adenine analogue was found to be the most cytotoxic...