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Page 1
Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease.
Keenan M, Abbott MJ, Alexander PW, Armstrong T, Best WM, Berven B, Botero A, Chaplin JH, Charman SA, Chatelain E, von Geldern TW, Kerfoot M, Khong A, Nguyen T, McManus JD, Morizzi J, Ryan E, Scandale I, Thompson RA, Wang SZ, White KL. Keenan M, et al. Among authors: von geldern tw. J Med Chem. 2012 May 10;55(9):4189-204. doi: 10.1021/jm2015809. Epub 2012 Apr 27. J Med Chem. 2012. PMID: 22536986
Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi.
Keenan M, Alexander PW, Diao H, Best WM, Khong A, Kerfoot M, Thompson RC, White KL, Shackleford DM, Ryan E, Gregg AD, Charman SA, von Geldern TW, Scandale I, Chatelain E. Keenan M, et al. Among authors: von geldern tw. Bioorg Med Chem. 2013 Apr 1;21(7):1756-63. doi: 10.1016/j.bmc.2013.01.050. Epub 2013 Jan 31. Bioorg Med Chem. 2013. PMID: 23462713 Free article.
Two analogues of fenarimol show curative activity in an experimental model of Chagas disease.
Keenan M, Chaplin JH, Alexander PW, Abbott MJ, Best WM, Khong A, Botero A, Perez C, Cornwall S, Thompson RA, White KL, Shackleford DM, Koltun M, Chiu FC, Morizzi J, Ryan E, Campbell M, von Geldern TW, Scandale I, Chatelain E, Charman SA. Keenan M, et al. Among authors: von geldern tw. J Med Chem. 2013 Dec 27;56(24):10158-70. doi: 10.1021/jm401610c. Epub 2013 Dec 4. J Med Chem. 2013. PMID: 24304150 Free PMC article.
Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts.
Le Manach C, Dam J, Woodland JG, Kaur G, Khonde LP, Brunschwig C, Njoroge M, Wicht KJ, Horatscheck A, Paquet T, Boyle GA, Gibhard L, Taylor D, Lawrence N, Yeo T, Mok S, Eastman RT, Dorjsuren D, Talley DC, Guo H, Simeonov A, Reader J, van der Watt M, Erlank E, Venter N, Zawada JW, Aswat A, Nardini L, Coetzer TL, Lauterbach SB, Bezuidenhout BC, Theron A, Mancama D, Koekemoer LL, Birkholtz LM, Wittlin S, Delves M, Ottilie S, Winzeler EA, von Geldern TW, Smith D, Fidock DA, Street LJ, Basarab GS, Duffy J, Chibale K. Le Manach C, et al. Among authors: von geldern tw. J Med Chem. 2021 Feb 25;64(4):2291-2309. doi: 10.1021/acs.jmedchem.1c00034. Epub 2021 Feb 12. J Med Chem. 2021. PMID: 33573376
New antimitotic agents with activity in multi-drug-resistant cell lines and in vivo efficacy in murine tumor models.
Szczepankiewicz BG, Liu G, Jae HS, Tasker AS, Gunawardana IW, von Geldern TW, Gwaltney SL 2nd, Wu-Wong JR, Gehrke L, Chiou WJ, Credo RB, Alder JD, Nukkala MA, Zielinski NA, Jarvis K, Mollison KW, Frost DJ, Bauch JL, Hui YH, Claiborne AK, Li Q, Rosenberg SH. Szczepankiewicz BG, et al. Among authors: von geldern tw. J Med Chem. 2001 Dec 6;44(25):4416-30. doi: 10.1021/jm010231w. J Med Chem. 2001. PMID: 11728187
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Pei Z, Li X, von Geldern TW, Madar DJ, Longenecker K, Yong H, Lubben TH, Stewart KD, Zinker BA, Backes BJ, Judd AS, Mulhern M, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Reinhart GA, Fryer RM, Preusser LC, Kempf-Grote AJ, Sham HL, Trevillyan JM. Pei Z, et al. Among authors: von geldern tw. J Med Chem. 2006 Nov 2;49(22):6439-42. doi: 10.1021/jm060955d. J Med Chem. 2006. PMID: 17064063
Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 1. Identification of an additional binding pocket based on an anilino diaryl sulfide lead.
Liu G, Link JT, Pei Z, Reilly EB, Leitza S, Nguyen B, Marsh KC, Okasinski GF, von Geldern TW, Ormes M, Fowler K, Gallatin M. Liu G, et al. Among authors: von geldern tw. J Med Chem. 2000 Oct 19;43(21):4025-40. doi: 10.1021/jm0002782. J Med Chem. 2000. PMID: 11052808
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.
Madar DJ, Kopecka H, Pireh D, Yong H, Pei Z, Li X, Wiedeman PE, Djuric SW, Von Geldern TW, Fickes MG, Bhagavatula L, McDermott T, Wittenberger S, Richards SJ, Longenecker KL, Stewart KD, Lubben TH, Ballaron SJ, Stashko MA, Long MA, Wells H, Zinker BA, Mika AK, Beno DW, Kempf-Grote AJ, Polakowski J, Segreti J, Reinhart GA, Fryer RM, Sham HL, Trevillyan JM. Madar DJ, et al. Among authors: von geldern tw. J Med Chem. 2006 Oct 19;49(21):6416-20. doi: 10.1021/jm060777o. J Med Chem. 2006. PMID: 17034148
Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.
Pei Z, Li X, von Geldern TW, Longenecker K, Pireh D, Stewart KD, Backes BJ, Lai C, Lubben TH, Ballaron SJ, Beno DW, Kempf-Grote AJ, Sham HL, Trevillyan JM. Pei Z, et al. Among authors: von geldern tw. J Med Chem. 2007 Apr 19;50(8):1983-7. doi: 10.1021/jm061436d. Epub 2007 Mar 17. J Med Chem. 2007. PMID: 17367123
66 results