| Year |
Citation |
Score |
| 2024 |
Huang G, Jung A, Li LX, Do N, Jung S, Jeon Y, Zuo D, Thanh La M, Van Manh N, Blumberg PM, Yoon H, Lee Y, Ann J, Lee J. Discovery of N-(1,4-Benzoxazin-3-one) urea analogs as Mode-Selective TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters. 129735. PMID 38588785 DOI: 10.1016/j.bmcl.2024.129735 |
0.489 |
|
| 2024 |
Zuo D, Hong M, Jung A, Lee S, Do N, Jung S, Jeon Y, Won Jeong J, Huang G, Li LX, Blumberg PM, Yoon H, Lee Y, Ann J, Lee J. Discovery of N-(1-(2-hydroxyethyl)quinolin-2-one)-N'-(1-phenyl-1H-pyrazol-5-yl)methyl) urea as Mode-Selective TRPV1 antagonist. Bioorganic & Medicinal Chemistry Letters. 129656. PMID 38355061 DOI: 10.1016/j.bmcl.2024.129656 |
0.695 |
|
| 2023 |
Das J, You Y, Mathukumalli K, Ann J, Lee J, Marquez VE. Activation of Munc13-1 by Diacylglycerol (DAG)-Lactones. Biochemistry. PMID 37651159 DOI: 10.1021/acs.biochem.3c00375 |
0.341 |
|
| 2023 |
Huang G, Hoang VH, Min HY, Lee HY, Ann J, Lee J. Syntheses and Antitumor Activities of Neorautenol and Shinpterocarpin Analogs. Bioorganic & Medicinal Chemistry Letters. 129353. PMID 37271378 DOI: 10.1016/j.bmcl.2023.129353 |
0.331 |
|
| 2022 |
Jung J, Lee Y, Moon AN, Ann J, Jeong JJ, Do N, Lee J. Discovery of Novel Dual Adenosine A and A Receptor Antagonists with 1-Pyrazolo[3,4]pyrimidin-6-amine Core Scaffold as Anti-Parkinson's Disease Agents. Pharmaceuticals (Basel, Switzerland). 15. PMID 35893746 DOI: 10.3390/ph15080922 |
0.341 |
|
| 2022 |
Zuo D, Do N, Hwang I, Ann J, Yu JW, Lee J. Design and Synthesis of an N-Benzyl 5-(4-Sulfamoylbenzylidene-2-thioxothiazolidin-4-one Scaffold as a Novel NLRP3 Inflammasome Inhibitor. Bioorganic & Medicinal Chemistry Letters. 128693. PMID 35314328 DOI: 10.1016/j.bmcl.2022.128693 |
0.403 |
|
| 2022 |
Lee HJ, Min HY, Yong YS, Ann J, Nguyen CT, La MT, Hyun SY, Le HT, Kim H, Kwon H, Nam G, Park HJ, Lee J, Lee HY. A novel C-terminal heat shock protein 90 inhibitor that overcomes STAT3-Wnt-β-catenin signaling-mediated drug resistance and adverse effects. Theranostics. 12: 105-125. PMID 34987637 DOI: 10.7150/thno.63788 |
0.354 |
|
| 2021 |
Linciano P, Nasti R, Listro R, Amadio M, Pascale A, Potenza D, Vasile F, Minneci M, Ann J, Lee J, Zhou X, Mitchell GA, Blumberg PM, Rossi D, Collina S. Chiral 2-phenyl-3-hydroxypropyl esters as PKC-alpha modulators: HPLC enantioseparation, NMR absolute configuration assignment, and molecular docking studies. Chirality. PMID 34962318 DOI: 10.1002/chir.23406 |
0.341 |
|
| 2021 |
Kang JM, Kwon SO, Ann J, Lee S, Kim C, Do N, Jeong JJ, Blumberg PM, Ha H, Vu TNL, Yoon S, Choi S, Frank-Foltyn R, Lesch B, Bahrenberg G, ... ... Lee J, et al. 2-(Halogenated Phenyl) Acetamides and Propanamides as Potent TRPV1 Antagonists. Bioorganic & Medicinal Chemistry Letters. 128266. PMID 34273488 DOI: 10.1016/j.bmcl.2021.128266 |
0.411 |
|
| 2021 |
Nguyen CT, Thanh La M, Ann J, Nam G, Park HJ, Min Park J, Kim YJ, Young Kim J, Hong Seo J, Lee J. Discovery of a simplified deguelin analog as an HSP90 C-terminal inhibitor for HER2-positive breast cancer. Bioorganic & Medicinal Chemistry Letters. 45: 128134. PMID 34044120 DOI: 10.1016/j.bmcl.2021.128134 |
0.442 |
|
| 2021 |
Jung J, Yoon H, Sohn TI, Jang K, Yoo Y, Jeong I, Shin JE, Lee JH, Ann J, Lee J. Discovery of 5-(N-Hydroxycarbamimidoyl) Benzofuran Derivatives as Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors. Bioorganic & Medicinal Chemistry Letters. 127963. PMID 33741464 DOI: 10.1016/j.bmcl.2021.127963 |
0.346 |
|
| 2020 |
Mi Kang J, Ok Kwon S, Ann J, Blumberg PM, Ha H, Dong Yoo Y, Frank-Foltyn R, Lesch B, Bahrenberg G, Stockhausen H, Christoph T, Lee J. Discovery of 1-(1H-Indazol-4-yl)-3-((1-Phenyl-1H-Pyrazol-5-yl)methyl) Ureas as Potent and Thermoneutral TRPV1 Antagonists. Bioorganic & Medicinal Chemistry Letters. 127548. PMID 32931910 DOI: 10.1016/j.bmcl.2020.127548 |
0.417 |
|
| 2020 |
Nguyen CT, Ann J, Sahu R, Byun WS, Lee S, Nam G, Park HJ, Park S, Kim YJ, Kim JY, Seo JH, Lee J. Discovery of novel anti-breast cancer agents derived from deguelin as inhibitors of heat shock protein 90 (HSP90). Bioorganic & Medicinal Chemistry Letters. 30: 127374. PMID 32738983 DOI: 10.1016/j.bmcl.2020.127374 |
0.391 |
|
| 2020 |
Jung J, Kwon J, Hong S, Moon AN, Jeong J, Kwon S, Kim JA, Lee M, Lee H, Lee JH, Lee J. Discovery of novel heat shock protein (Hsp90) inhibitors based on luminespib with potent antitumor activity. Bioorganic & Medicinal Chemistry Letters. 127165. PMID 32305165 DOI: 10.1016/j.bmcl.2020.127165 |
0.375 |
|
| 2019 |
Ahn S, Kim YS, Kim MS, Ann J, Ha H, Yoo YD, Kim YH, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J. Discovery of indane propanamides as potent and selective TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters. 126838. PMID 31864799 DOI: 10.1016/J.Bmcl.2019.126838 |
0.307 |
|
| 2019 |
Lee HR, Kang JM, Kim YM, Kim S, Ann J, Lee J, Kim HJ. Functional Group-Dependent Induction of Astrocytogenesis and Neurogenesis by Flavone Derivatives. Biomolecules. 9. PMID 31810286 DOI: 10.3390/biom9120812 |
0.347 |
|
| 2019 |
Hoang VH, Ngo VTH, Cui M, Manh NV, Tran PT, Ann J, Ha H, Kim H, Choi K, Kim YH, Chang H, Macalino SJY, Lee J, Choi S, Lee J. Discovery of Conformationally Restricted Human Glutaminyl Cyclase Inhibitors as Potent Anti-Alzheimer's Agents by Structure-Based Design. Journal of Medicinal Chemistry. PMID 31411468 DOI: 10.1021/Acs.Jmedchem.9B00751 |
0.367 |
|
| 2019 |
Kim HS, Hoang VH, Hong M, Chul Kim K, Ann J, Nguyen CT, Seo JH, Choi H, Yong Kim J, Kim KW, Sub Byun W, Lee S, Lee S, Suh YG, Chen J, ... ... Lee J, et al. Investigation of B,C-ring truncated deguelin derivatives as heat shock protein 90 (HSP90) inhibitors for use as anti-breast cancer agents. Bioorganic & Medicinal Chemistry. PMID 30827868 DOI: 10.1016/j.bmc.2019.02.040 |
0.72 |
|
| 2019 |
Yoon S, Kim SE, Kim JH, Yoon I, Tran PT, Ann J, Kim C, Byun WS, Lee S, Kim S, Lee J, Lee J. Structure-activity relationship of leucyladenylate sulfamate analogues as leucyl-tRNA synthetase (LRS)-targeting inhibitors of Mammalian target of rapamycin complex 1 (mTORC1). Bioorganic & Medicinal Chemistry. PMID 30755350 DOI: 10.1016/J.Bmc.2019.01.037 |
0.305 |
|
| 2018 |
An H, Lee S, Lee JM, Jo DH, Kim J, Jeong YS, Heo MJ, Cho CS, Choi H, Seo JH, Hwang S, Lim J, Kim T, Jun HO, Sim J, ... ... Lee J, ... ... Lee J, et al. Novel Hypoxia-Inducible Factor 1α (HIF-1α) Inhibitors for Angiogenesis-Related Ocular Diseases: Discovery of a Novel Scaffold via Ring-Truncation Strategy. Journal of Medicinal Chemistry. PMID 30252468 DOI: 10.1021/Acs.Jmedchem.8B00971 |
0.415 |
|
| 2018 |
Kim C, Ann J, Lee S, Kim E, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J. 4-Aminophenyl acetamides and propanamides as potent transient receptor potential vanilloid 1 (TRPV1) ligands. Bioorganic & Medicinal Chemistry. PMID 30078610 DOI: 10.1016/J.Bmc.2018.07.040 |
0.374 |
|
| 2018 |
Yoon S, Zuo D, Kim JH, Yoon I, Ann J, Kim SE, Cho D, Kim WK, Lee S, Lee J, Kim S, Lee J. Discovery of novel leucyladenylate sulfamate surrogates as leucyl-tRNA synthetase (LRS)-targeted mammalian target of rapamycin complex 1 (mTORC1) inhibitors. Bioorganic & Medicinal Chemistry. PMID 30041947 DOI: 10.1016/J.Bmc.2018.06.034 |
0.304 |
|
| 2018 |
Kim C, Ann J, Lee S, Sun W, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J. Discovery of 2-(3,5-difluoro-4-methylsulfonaminophenyl)propanamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters. PMID 29884534 DOI: 10.1016/J.Bmcl.2018.05.043 |
0.36 |
|
| 2018 |
Ann J, Czikora A, Saini A, Zhou X, Mitchell GA, Lewin NE, Peach ML, Blumberg PM, Lee J. α-Arylidene Diacylglycerol-Lactones (DAG-Lactones) as Selective Ras Guanine Releasing Protein 3 (RasGRP3) Ligands. Journal of Medicinal Chemistry. PMID 29860841 DOI: 10.1021/Acs.Jmedchem.8B00661 |
0.367 |
|
| 2018 |
Ngo VTH, Hoang VH, Tran PT, Van Manh N, Ann J, Kim E, Cui M, Choi S, Lee J, Kim H, Ha HJ, Choi K, Kim YH, Lee J. Structure-activity relationship investigation of Phe-Arg mimetic region of human glutaminyl cyclase inhibitors. Bioorganic & Medicinal Chemistry. PMID 29705377 DOI: 10.1016/J.Bmc.2018.04.040 |
0.417 |
|
| 2018 |
Cooke M, Zhou X, Casado-Medrano V, Lopez-Haber C, Baker MJ, Garg R, Ann J, Lee J, Blumberg PM, Kazanietz MG. Characterization of AJH-836, a DAG-lactone with selectivity for novel PKC isozymes. The Journal of Biological Chemistry. PMID 29636415 DOI: 10.1074/Jbc.Ra117.000235 |
0.313 |
|
| 2018 |
Ngo VTH, Hoang VH, Tran PT, Ann J, Cui M, Park G, Choi S, Lee J, Kim H, Ha HJ, Choi K, Kim YH, Lee J. Potent human glutaminyl cyclase inhibitors as potential anti-Alzheimer's agents: Structure-activity relationship study of Arg-mimetic region. Bioorganic & Medicinal Chemistry. PMID 29398442 DOI: 10.1016/J.Bmc.2018.01.015 |
0.343 |
|
| 2018 |
Kim SM, Lee M, Lee SY, Lee SM, Kim EJ, Kim JS, Ann J, Lee J, Lee J. Synthesis and biological evaluation of 3-(2-aminoethyl) uracil derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists. European Journal of Medicinal Chemistry. 145: 413-424. PMID 29335207 DOI: 10.1016/J.Ejmech.2017.12.095 |
0.427 |
|
| 2017 |
Lee S, Kim C, Ann J, Thorat SA, Kim E, Park J, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J. Pyrazole C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters. PMID 28838698 DOI: 10.1016/J.Bmcl.2017.08.020 |
0.51 |
|
| 2017 |
Lee S, Kang DW, Ryu H, Kim C, Ann J, Lee H, Kim E, Hong S, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J. t-Butyl pyridine and phenyl C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry. PMID 28314510 DOI: 10.1016/J.Bmc.2017.03.004 |
0.444 |
|
| 2016 |
Kim HS, Hong M, Ann J, Yoon S, Nguyen CT, Lee SC, Lee HY, Suh YG, Seo JH, Choi H, Kim JY, Kim KW, Kim J, Kim YM, Park SJ, ... ... Lee J, et al. Synthesis and biological evaluation of C-ring truncated deguelin derivatives as heat shock protein 90 (HSP90) inhibitors. Bioorganic & Medicinal Chemistry. PMID 27745993 DOI: 10.1016/j.bmc.2016.09.067 |
0.733 |
|
| 2016 |
Ann J, Sun W, Zhou X, Jung A, Baek J, Lee S, Kim C, Yoon S, Hong S, Choi S, Turcios NA, Herold BK, Esch TE, Lewin NE, Abramovitz A, ... ... Lee J, et al. Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template. Bioorganic & Medicinal Chemistry Letters. PMID 27317643 DOI: 10.1016/J.Bmcl.2016.06.010 |
0.427 |
|
| 2016 |
Yoon S, Kim JH, Yoon I, Kim C, Kim SE, Koh Y, Jeong SJ, Lee J, Kim S, Lee J. Discovery of (S)-4-isobutyloxazolidin-2-one as a novel leucyl-tRNA synthetase (LRS)-targeted mTORC1 inhibitor. Bioorganic & Medicinal Chemistry Letters. PMID 27209231 DOI: 10.1016/J.Bmcl.2016.05.011 |
0.371 |
|
| 2016 |
Ann J, Ki Y, Yoon S, Kim MS, Lee JU, Kim C, Lee S, Jung A, Baek J, Hong S, Choi S, Pearce LV, Esch TE, Turcios NA, Lewin NE, ... ... Lee J, et al. 2-Sulfonamidopyridine C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry. PMID 26860926 DOI: 10.1016/J.Bmc.2016.01.051 |
0.473 |
|
| 2015 |
Ann J, Jung A, Kim MY, Kim HM, Ryu H, Kim S, Kang DW, Hong S, Cui M, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, ... Lee J, et al. Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry. PMID 26474664 DOI: 10.1016/J.Bmc.2015.10.001 |
0.526 |
|
| 2015 |
Kim HS, Hong M, Lee SC, Lee HY, Suh YG, Oh DC, Seo JH, Choi H, Kim JY, Kim KW, Kim JH, Kim J, Kim YM, Park SJ, Park HJ, ... Lee J, et al. Ring-truncated deguelin derivatives as potent Hypoxia Inducible Factor-1α (HIF-1α) inhibitors. European Journal of Medicinal Chemistry. 104: 157-164. PMID 26457742 DOI: 10.1016/j.ejmech.2015.09.033 |
0.732 |
|
| 2015 |
Lee SC, Min HY, Choi H, Kim HS, Kim KC, Park SJ, Seong MA, Seo JH, Park HJ, Suh YG, Kim KW, Hong HS, Kim H, Lee MY, Lee J, et al. Synthesis and Evaluation of a Novel Deguelin Derivative, L80, which Disrupts ATP Binding to the C-terminal Domain of Heat Shock Protein 90. Molecular Pharmacology. 88: 245-55. PMID 25976766 DOI: 10.1124/mol.114.096883 |
0.352 |
|
| 2015 |
Tran PT, Kim HS, Ann J, Kim SE, Kim C, Hong M, Hoang VH, Ngo VT, Hong S, Cui M, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, ... ... Lee J, et al. α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters. 25: 2326-30. PMID 25937016 DOI: 10.1016/J.Bmcl.2015.04.024 |
0.703 |
|
| 2015 |
Ryu H, Seo S, Lee JY, Ha TH, Lee S, Jung A, Ann J, Kim SE, Yoon S, Hong M, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Schiene K, Stockhausen H, ... ... Lee J, et al. Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists. European Journal of Medicinal Chemistry. 93: 101-8. PMID 25659771 DOI: 10.1016/J.Ejmech.2015.02.001 |
0.707 |
|
| 2015 |
Sun W, Kim HS, Lee S, Jung A, Kim SE, Ann J, Yoon S, Choi S, Lee JH, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Schiene K, Stockhausen H, Christoph T, ... ... Lee J, et al. 6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters. 25: 803-6. PMID 25597011 DOI: 10.1016/J.Bmcl.2014.12.086 |
0.387 |
|
| 2015 |
Han YT, Kim K, Son D, An H, Kim H, Lee J, Park HJ, Lee J, Suh YG. Fine tuning of 4,6-bisphenyl-2-(3-alkoxyanilino)pyrimidine focusing on the activity-sensitive aminoalkoxy moiety for a therapeutically useful inhibitor of receptor for advanced glycation end products (RAGE). Bioorganic & Medicinal Chemistry. 23: 579-87. PMID 25533401 DOI: 10.1016/j.bmc.2014.12.003 |
0.39 |
|
| 2014 |
Ryu H, Seo S, Kim MS, Kim MY, Kim HS, Ann J, Tran PT, Hoang VH, Byun J, Cui M, Son K, Sharma PK, Choi S, Blumberg PM, Frank-Foltyn R, ... ... Lee J, et al. 2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters. 24: 4044-7. PMID 25011915 DOI: 10.1016/J.Bmcl.2014.05.072 |
0.506 |
|
| 2014 |
Ryu H, Seo S, Cho SH, Kim HS, Jung A, Kang DW, Son K, Cui M, Hong SH, Sharma PK, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, ... ... Lee J, et al. 2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters. 24: 4039-43. PMID 24948568 DOI: 10.1016/j.bmcl.2014.05.074 |
0.442 |
|
| 2014 |
Jo DH, An H, Chang DJ, Baek YY, Cho CS, Jun HO, Park SJ, Kim JH, Lee HY, Kim KW, Lee J, Park HJ, Kim YM, Suh YG, Kim JH. Hypoxia-mediated retinal neovascularization and vascular leakage in diabetic retina is suppressed by HIF-1α destabilization by SH-1242 and SH-1280, novel hsp90 inhibitors. Journal of Molecular Medicine (Berlin, Germany). 92: 1083-92. PMID 24875598 DOI: 10.1007/s00109-014-1168-8 |
0.302 |
|
| 2014 |
Kim HS, Jin MK, Kang SU, Lim JO, Tran PT, Hoang VH, Ann J, Ha TH, Pearce LV, Pavlyukovets VA, Blumberg PM, Lee J. α-Methylated simplified resiniferatoxin (sRTX) thiourea analogues as potent and stereospecific TRPV1 antagonists. Bioorganic & Medicinal Chemistry Letters. 24: 2685-8. PMID 24794110 DOI: 10.1016/J.Bmcl.2014.04.054 |
0.444 |
|
| 2014 |
Han YT, Kim K, Choi GI, An H, Son D, Kim H, Ha HJ, Son JH, Chung SJ, Park HJ, Lee J, Suh YG. Pyrazole-5-carboxamides, novel inhibitors of receptor for advanced glycation end products (RAGE). European Journal of Medicinal Chemistry. 79: 128-42. PMID 24727489 DOI: 10.1016/j.ejmech.2014.03.072 |
0.327 |
|
| 2014 |
Kim MS, Ki Y, Ahn SY, Yoon S, Kim SE, Park HG, Sun W, Son K, Cui M, Choi S, Pearce LV, Esch TE, Deandrea-Lazarus IA, Blumberg PM, Lee J. Asymmetric synthesis and receptor activity of chiral simplified resiniferatoxin (sRTX) analogues as transient receptor potential vanilloid 1 (TRPV1) ligands. Bioorganic & Medicinal Chemistry Letters. 24: 382-5. PMID 24321344 DOI: 10.1016/J.Bmcl.2013.10.064 |
0.32 |
|
| 2013 |
Ha TH, Ryu H, Kim SE, Kim HS, Ann J, Tran PT, Hoang VH, Son K, Cui M, Choi S, Blumberg PM, Frank R, Bahrenberg G, Schiene K, Christoph T, ... ... Lee J, et al. TRPV1 antagonist with high analgesic efficacy: 2-Thio pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides. Bioorganic & Medicinal Chemistry. 21: 6657-64. PMID 24035514 DOI: 10.1016/J.Bmc.2013.08.015 |
0.477 |
|
| 2013 |
Thorat SA, Kang DW, Ryu H, Kim MS, Kim HS, Ann J, Ha T, Kim SE, Son K, Choi S, Blumberg PM, Frank R, Bahrenberg G, Schiene K, Christoph T, ... Lee J, et al. 2-(3-Fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists: structure activity relationships of the 2-oxy pyridine C-region. European Journal of Medicinal Chemistry. 64: 589-602. PMID 23685943 DOI: 10.1016/J.Ejmech.2013.04.003 |
0.516 |
|
| 2013 |
Tran PT, Hoang VH, Thorat SA, Kim SE, Ann J, Chang YJ, Nam DW, Song H, Mook-Jung I, Lee J, Lee J. Structure-activity relationship of human glutaminyl cyclase inhibitors having an N-(5-methyl-1H-imidazol-1-yl)propyl thiourea template. Bioorganic & Medicinal Chemistry. 21: 3821-30. PMID 23643900 DOI: 10.1016/J.Bmc.2013.04.005 |
0.441 |
|
| 2012 |
Kim MS, Ryu H, Kang DW, Cho SH, Seo S, Park YS, Kim MY, Kwak EJ, Kim YS, Bhondwe RS, Kim HS, Park SG, Son K, Choi S, DeAndrea-Lazarus IA, ... ... Lee J, et al. 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent transient receptor potential vanilloid 1 (TRPV1) antagonists: structure-activity relationships of 2-amino derivatives in the N-(6-trifluoromethylpyridin-3-ylmethyl) C-region. Journal of Medicinal Chemistry. 55: 8392-408. PMID 22957803 DOI: 10.1021/Jm300780P |
0.496 |
|
| 2012 |
Cho Y, Kim MS, Kim HS, Ann J, Lee J, Pearce LV, Pavlyukovets VA, Morgan MA, Blumberg PM, Lee J. The SAR analysis of TRPV1 agonists with the α-methylated B-region. Bioorganic & Medicinal Chemistry Letters. 22: 5227-31. PMID 22796184 DOI: 10.1016/J.Bmcl.2012.06.059 |
0.374 |
|
| 2012 |
Han YT, Choi GI, Son D, Kim NJ, Yun H, Lee S, Chang DJ, Hong HS, Kim H, Ha HJ, Kim YH, Park HJ, Lee J, Suh YG. Ligand-based design, synthesis, and biological evaluation of 2-aminopyrimidines, a novel series of receptor for advanced glycation end products (RAGE) inhibitors. Journal of Medicinal Chemistry. 55: 9120-35. PMID 22742537 DOI: 10.1021/Jm300172Z |
0.315 |
|
| 2012 |
Bhondwe RS, Kang DW, Kim MS, Kim HS, Park SG, Son K, Choi S, Kuhs KA, Pavlyukovets VA, Pearce LV, Blumberg PM, Lee J. Structure-activity relationships and molecular modeling of the N-(3-pivaloyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl] thiourea template for TRPV1 antagonism. Bioorganic & Medicinal Chemistry Letters. 22: 3656-60. PMID 22546668 DOI: 10.1016/J.Bmcl.2012.04.034 |
0.341 |
|
| 2012 |
Sun W, Liu K, Ryu H, Kang DW, Kim YS, Kim MS, Cho Y, Bhondwe RS, Thorat SA, Kim HS, Pearce LV, Pavlyukovets VA, Tran R, Morgan MA, Lazar J, ... ... Lee J, et al. 2-(4-Methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the B and C-regions. Bioorganic & Medicinal Chemistry. 20: 1310-8. PMID 22227463 DOI: 10.1016/J.Bmc.2011.12.014 |
0.459 |
|
| 2012 |
Kim YS, Kil MJ, Kang SU, Ryu H, Kim MS, Cho Y, Bhondwe RS, Thorat SA, Sun W, Liu K, Lee JH, Choi S, Pearce LV, Pavlyukovets VA, Morgan MA, ... ... Lee J, et al. N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region. Bioorganic & Medicinal Chemistry. 20: 215-24. PMID 22169633 DOI: 10.1016/J.Bmc.2011.11.008 |
0.341 |
|
| 2011 |
Lim KS, Kang DW, Kim YS, Kim MS, Park SG, Choi S, Pearce LV, Blumberg PM, Lee J. Receptor activity and conformational analysis of 5'-halogenated resiniferatoxin analogs as TRPV1 ligands. Bioorganic & Medicinal Chemistry Letters. 21: 299-302. PMID 21111618 DOI: 10.1016/J.Bmcl.2010.11.012 |
0.439 |
|
| 2010 |
Kang DW, Kim YS, Lim KS, Kim MS, Pearce LV, Pavlyukovets VA, Tao AK, Lang-Kuhs KA, Blumberg PM, Lee J. Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin. Bioorganic & Medicinal Chemistry. 18: 8092-105. PMID 20937561 DOI: 10.1016/J.Bmc.2010.09.001 |
0.411 |
|
| 2010 |
Kang JH, Kim Y, Won SH, Park SK, Lee CW, Kim HM, Lewin NE, Perry NA, Pearce LV, Lundberg DJ, Surawski RJ, Blumberg PM, Lee J. Polar 3-alkylidene-5-pivaloyloxymethyl-5'-hydroxymethyl-gamma-lactones as protein kinase C ligands and antitumor agents. Bioorganic & Medicinal Chemistry Letters. 20: 1008-12. PMID 20045644 DOI: 10.1016/J.Bmcl.2009.12.058 |
0.326 |
|
| 2009 |
Choi HK, Choi S, Lee Y, Kang DW, Ryu H, Maeng HJ, Chung SJ, Pavlyukovets VA, Pearce LV, Toth A, Tran R, Wang Y, Morgan MA, Blumberg PM, Lee J. Non-vanillyl resiniferatoxin analogues as potent and metabolically stable transient receptor potential vanilloid 1 agonists. Bioorganic & Medicinal Chemistry. 17: 690-8. PMID 19135377 DOI: 10.1016/J.Bmc.2008.11.085 |
0.378 |
|
| 2009 |
Lim JO, Jin MK, Ryu H, Kang DW, Lee J, Pearce LV, Tran R, Toth A, Blumberg PM. Conformationally constrained analogues of N'-(4-tert-butylbenzyl)-N-(4-methylsulfonylaminobenzyl)thiourea as TRPV1 antagonists. European Journal of Medicinal Chemistry. 44: 322-31. PMID 18406014 DOI: 10.1016/J.Ejmech.2008.02.026 |
0.36 |
|
| 2009 |
Farhanullah, Kang T, Yoon E, Choi E, Kim S, Lee J. 2-[2-Substituted-3-(3,4-dichlorobenzylamino)propylamino]-1H-quinolin-4-ones as Staphylococcus aureus methionyl-tRNA synthetase inhibitors European Journal of Medicinal Chemistry. 44: 239-250. PMID 18403059 DOI: 10.1016/J.Ejmech.2008.02.021 |
0.363 |
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| 2008 |
Pearce LV, Toth A, Ryu H, Kang DW, Choi HK, Jin MK, Lee J, Blumberg PM. Differential modulation of agonist and antagonist structure activity relations for rat TRPV1 by cyclosporin A and other protein phosphatase inhibitors. Naunyn-Schmiedeberg's Archives of Pharmacology. 377: 149-57. PMID 18259730 DOI: 10.1007/S00210-007-0258-3 |
0.311 |
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| 2008 |
Ryu H, Jin MK, Kim SY, Choi HK, Kang SU, Kang DW, Lee J, Pearce LV, Pavlyukovets VA, Morgan MA, Tran R, Toth A, Lundberg DJ, Blumberg PM. Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues. Journal of Medicinal Chemistry. 51: 57-67. PMID 18072720 DOI: 10.1021/Jm701049P |
0.404 |
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| 2007 |
Kang DW, Ryu H, Lee J, Lang KA, Pavlyukovets VA, Pearce LV, Ikeda T, Lazar J, Blumberg PM. Halogenation of 4-hydroxy-3-methoxybenzyl thiourea TRPV1 agonists showed enhanced antagonism to capsaicin. Bioorganic & Medicinal Chemistry Letters. 17: 214-9. PMID 17035013 DOI: 10.1016/J.Bmcl.2006.09.059 |
0.402 |
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| 2006 |
Farhanullah, Kim SY, Yoon EJ, Choi EC, Kim S, Kang T, Samrin F, Puri S, Lee J. Design and synthesis of quinolinones as methionyl-tRNA synthetase inhibitors. Bioorganic & Medicinal Chemistry. 14: 7154-9. PMID 16854585 DOI: 10.1016/J.Bmc.2006.06.062 |
0.323 |
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| 2006 |
Kim SY, Lee Y, Kang T, Kim S, Lee J. Pharmacophore-based virtual screening: the discovery of novel methionyl-tRNA synthetase inhibitors. Bioorganic & Medicinal Chemistry Letters. 16: 4898-4907. PMID 16824759 DOI: 10.1016/J.Bmcl.2006.06.057 |
0.305 |
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| 2006 |
Lee J, Kang JH, Han KC, Kim Y, Kim SY, Youn HS, Mook-Jung I, Kim H, Lo Han JH, Ha HJ, Kim YH, Marquez VE, Lewin NE, Pearce LV, Lundberg DJ, et al. Branched diacylglycerol-lactones as potent protein kinase C ligands and alpha-secretase activators. Journal of Medicinal Chemistry. 49: 2028-36. PMID 16539391 DOI: 10.1021/Jm0509391 |
0.316 |
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| 2006 |
Lee J, Lee JH, Kim SY, Perry NA, Lewin NE, Ayres JA, Blumberg PM. 2-Benzyl and 2-phenyl-3-hydroxypropyl pivalates as protein kinase C ligands. Bioorganic & Medicinal Chemistry. 14: 2022-31. PMID 16297629 DOI: 10.1016/J.Bmc.2005.10.051 |
0.381 |
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| 2005 |
Suh YG, Lee YS, Min KH, Park OH, Kim JK, Seung HS, Seo SY, Lee BY, Nam YH, Lee KO, Kim HD, Park HG, Lee J, Oh U, Lim JO, et al. Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents. Journal of Medicinal Chemistry. 48: 5823-36. PMID 16134949 DOI: 10.1021/Jm0502790 |
0.302 |
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| 2004 |
Kang JH, Kim SY, Lee J, Marquez VE, Lewin NE, Pearce LV, Blumberg PM. Macrocyclic diacylglycerol-bis-lactones as conformationally constrained analogues of diacylglycerol-lactones. Interactions with protein kinase C. Journal of Medicinal Chemistry. 47: 4000-7. PMID 15267238 DOI: 10.1021/Jm0497747 |
0.422 |
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| 2004 |
Lee J, Kim SY, Lee J, Kang M, Kil MJ, Choi HK, Jin MK, Wang Y, Toth A, Pearce LV, Lundberg DJ, Tran R, Blumberg PM. Analysis of structure-activity relationships with the N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea template for vanilloid receptor 1 antagonism. Bioorganic & Medicinal Chemistry. 12: 3411-20. PMID 15186827 DOI: 10.1016/J.Bmc.2004.04.040 |
0.412 |
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| 2004 |
Kim SY, Lee J. 3D-QSAR analysis of conformationally constrained diacylglycerol (DAG) analogues as potent protein kinase C (PK-C) ligands. Bioorganic & Medicinal Chemistry. 12: 2639-44. PMID 15110845 DOI: 10.1016/j.bmc.2004.03.016 |
0.309 |
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| 2004 |
Lee J, Kang SU, Choi HK, Lee J, Lim JO, Kil MJ, Jin MK, Kim KP, Sung JH, Chung SJ, Ha HJ, Kim YH, Pearce LV, Tran R, Lundberg DJ, et al. Analysis of structure-activity relationships for the 'B-region' of N-(3-acyloxy-2-benzylpropyl)-N(')-[4-(methylsulfonylamino)benzyl]thiourea analogues as vanilloid receptor antagonists: discovery of an N-hydroxythiourea analogue with potent analgesic activity. Bioorganic & Medicinal Chemistry Letters. 14: 2291-7. PMID 15081027 DOI: 10.1016/J.Bmcl.2004.02.002 |
0.351 |
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| 2004 |
Ryu CH, Jang MJ, Jung JW, Park JH, Choi HY, Suh YG, Oh U, Park HG, Lee J, Koh HJ, Mo JH, Joo YH, Park YH, Kim HD. Chain-branched 1,3-dibenzylthioureas as vanilloid receptor 1 antagonists. Bioorganic & Medicinal Chemistry Letters. 14: 1751-5. PMID 15026064 DOI: 10.1016/J.Bmcl.2004.01.066 |
0.321 |
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| 2004 |
Lee J, Kim SY, Kang JH, Acs G, Acs P, Blumberg PM, Marquez VE. Conformationally constrained diacylglycerol (DAG) analogs: 4-C-hydroxyethyl-5-O-acyl-2,3-dideoxy-D-glyceropentono-1,4-lactone analogs as protein kinase C (PKC) ligands. European Journal of Medicinal Chemistry. 39: 69-77. PMID 14987835 DOI: 10.1016/J.Ejmech.2003.10.006 |
0.349 |
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| 2004 |
Lee J, Kim SY, Park S, Lim JO, Kim JM, Kang M, Lee J, Kang SU, Choi HK, Jin MK, Welter JD, Szabo T, Tran R, Pearce LV, Toth A, et al. Structure-activity relationships of simplified resiniferatoxin analogues with potent VR1 agonism elucidates an active conformation of RTX for VR1 binding. Bioorganic & Medicinal Chemistry. 12: 1055-69. PMID 14980619 DOI: 10.1016/J.Bmc.2003.12.005 |
0.393 |
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| 2004 |
Lee J, Kang SU, Lim JO, Choi HK, Jin MK, Toth A, Pearce LV, Tran R, Wang Y, Szabo T, Blumberg PM. N-[4-(methylsulfonylamino)benzyl]thiourea analogues as vanilloid receptor antagonists: analysis of structure-activity relationships for the "C-Region". Bioorganic & Medicinal Chemistry. 12: 371-85. PMID 14723956 DOI: 10.1016/J.Bmc.2003.10.047 |
0.344 |
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| 2003 |
Wang Y, Toth A, Tran R, Szabo T, Welter JD, Blumberg PM, Lee J, Kang SU, Lim JO, Lee J. High-affinity partial agonists of the vanilloid receptor. Molecular Pharmacology. 64: 325-33. PMID 12869637 DOI: 10.1124/Mol.64.2.325 |
0.388 |
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| 2003 |
Lee J, Lee J, Kang M, Shin M, Kim JM, Kang SU, Lim JO, Choi HK, Suh YG, Park HG, Oh U, Kim HD, Park YH, Ha HJ, Kim YH, et al. N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues: novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor. Journal of Medicinal Chemistry. 46: 3116-26. PMID 12825950 DOI: 10.1021/Jm030089U |
0.445 |
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| 2003 |
Kang JH, Chung HE, Kim SY, Kim Y, Lee J, Lewin NE, Pearce LV, Blumberg PM, Marquez VE. Conformationally constrained analogues of diacylglycerol (DAG). Effect on protein kinase C (PK-C) binding by the isosteric replacement of sn-1 and sn-2 esters in DAG-lactones Bioorganic and Medicinal Chemistry. 11: 2529-2539. PMID 12757721 DOI: 10.1016/S0968-0896(03)00156-1 |
0.395 |
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| 2003 |
Park Hg, Park Mk, Choi Jy, Choi Sh, Lee J, Suh Yg, Oh U, Lee J, Kim HD, Park YH, Jeong YS, Choi JK, Jew Ss. Synthesis of 2-substituted-pyrrolidinethiourea derivatives and their antagonist effect on vanilloid receptor. Bioorganic & Medicinal Chemistry Letters. 13: 197-200. PMID 12482422 DOI: 10.1016/S0960-894X(02)00887-9 |
0.304 |
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| 2002 |
Lee J, Lee J, Kang MS, Kim KP, Chung SJ, Blumberg PM, Yi JB, Park YH. Phenolic modification as an approach to improve the pharmacology of the 3-acyloxy-2-benzylpropyl homovanillic amides and thioureas, a promising class of vanilloid receptor agonists and analgesics. Bioorganic & Medicinal Chemistry. 10: 1171-9. PMID 11836128 DOI: 10.1016/S0968-0896(01)00387-X |
0.312 |
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