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A highly selective and potent CXCR4 antagonist for hepatocellular carcinoma treatment.
Song JS, Chang CC, Wu CH, Dinh TK, Jan JJ, Huang KW, Chou MC, Shiue TY, Yeh KC, Ke YY, Yeh TK, Ta YN, Lee CJ, Huang JK, Sung YC, Shia KS, Chen Y. Song JS, et al. Among authors: shia ks. Proc Natl Acad Sci U S A. 2021 Mar 30;118(13):e2015433118. doi: 10.1073/pnas.2015433118. Proc Natl Acad Sci U S A. 2021. PMID: 33753481 Free PMC article.
Bioisosteric replacement of the pyrazole 5-aryl moiety of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A). A novel series of alkynylthiophenes as potent and selective cannabinoid-1 receptor antagonists.
Tseng SL, Hung MS, Chang CP, Song JS, Tai CL, Chiu HH, Hsieh WP, Lin Y, Chung WL, Kuo CW, Wu CH, Chu CM, Tung YS, Chao YS, Shia KS. Tseng SL, et al. Among authors: shia ks. J Med Chem. 2008 Sep 11;51(17):5397-412. doi: 10.1021/jm800066v. Epub 2008 Aug 20. J Med Chem. 2008. PMID: 18712856
Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobesity efficacy in DIO mice.
Wu CH, Hung MS, Song JS, Yeh TK, Chou MC, Chu CM, Jan JJ, Hsieh MT, Tseng SL, Chang CP, Hsieh WP, Lin Y, Yeh YN, Chung WL, Kuo CW, Lin CY, Shy HS, Chao YS, Shia KS. Wu CH, et al. Among authors: shia ks. J Med Chem. 2009 Jul 23;52(14):4496-510. doi: 10.1021/jm900471u. J Med Chem. 2009. PMID: 19530697
Discovery of 1-(2,4-dichlorophenyl)-4-ethyl-5-(5-(2-(4-(trifluoromethyl)phenyl)ethynyl)thiophen-2-yl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide as a potential peripheral cannabinoid-1 receptor inverse agonist.
Hung MS, Chang CP, Li TC, Yeh TK, Song JS, Lin Y, Wu CH, Kuo PC, Amancha PK, Wong YC, Hsiao WC, Chao YS, Shia KS. Hung MS, et al. Among authors: shia ks. ChemMedChem. 2010 Sep 3;5(9):1439-43. doi: 10.1002/cmdc.201000246. ChemMedChem. 2010. PMID: 20652930 No abstract available.
Discovery of novel stem cell mobilizers that target the CXCR4 receptor.
Wu CH, Chang CP, Song JS, Jan JJ, Chou MC, Wu SH, Yeh KC, Wong YC, Hsieh CJ, Chen CT, Kao TT, Wu SY, Yeh CF, Tseng CT, Chao YS, Shia KS. Wu CH, et al. Among authors: shia ks. ChemMedChem. 2012 Feb 6;7(2):209-12. doi: 10.1002/cmdc.201100525. Epub 2011 Dec 20. ChemMedChem. 2012. PMID: 22190478 No abstract available.
Discovery of 1-(2,4-dichlorophenyl)-N-(piperidin-1-yl)-4-((pyrrolidine-1-sulfonamido)methyl)-5-(5-((4-(trifluoromethyl)phenyl)ethynyl)thiophene-2-yl)-1H-pyrazole-3-carboxamide as a novel peripherally restricted cannabinoid-1 receptor antagonist with significant weight-loss efficacy in diet-induced obese mice.
Chang CP, Wu CH, Song JS, Chou MC, Wong YC, Lin Y, Yeh TK, Sadani AA, Ou MH, Chen KH, Chen PH, Kuo PC, Tseng CT, Chang KH, Tseng SL, Chao YS, Hung MS, Shia KS. Chang CP, et al. Among authors: shia ks. J Med Chem. 2013 Dec 27;56(24):9920-33. doi: 10.1021/jm401158e. Epub 2013 Dec 4. J Med Chem. 2013. PMID: 24224693
Function-oriented development of CXCR4 antagonists as selective human immunodeficiency virus (HIV)-1 entry inhibitors.
Wu CH, Wang CJ, Chang CP, Cheng YC, Song JS, Jan JJ, Chou MC, Ke YY, Ma J, Wong YC, Hsieh TC, Tien YC, Gullen EA, Lo CF, Cheng CY, Liu YW, Sadani AA, Tsai CH, Hsieh HP, Tsou LK, Shia KS. Wu CH, et al. Among authors: shia ks. J Med Chem. 2015 Feb 12;58(3):1452-65. doi: 10.1021/jm501772w. Epub 2015 Jan 28. J Med Chem. 2015. PMID: 25584630 Free PMC article.
67 results