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Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists.
Lange JH, Coolen HK, van Stuivenberg HH, Dijksman JA, Herremans AH, Ronken E, Keizer HG, Tipker K, McCreary AC, Veerman W, Wals HC, Stork B, Verveer PC, den Hartog AP, de Jong NM, Adolfs TJ, Hoogendoorn J, Kruse CG. Lange JH, et al. Among authors: keizer hg. J Med Chem. 2004 Jan 29;47(3):627-43. doi: 10.1021/jm031019q. J Med Chem. 2004. PMID: 14736243
7-Azaindole derivatives as potential partial nicotinic agonists.
Stoit AR, den Hartog AP, Mons H, van Schaik S, Barkhuijsen N, Stroomer C, Coolen HK, Reinders JH, Adolfs TJ, van der Neut M, Keizer H, Kruse CG. Stoit AR, et al. Bioorg Med Chem Lett. 2008 Jan 1;18(1):188-93. doi: 10.1016/j.bmcl.2007.10.101. Epub 2007 Nov 1. Bioorg Med Chem Lett. 2008. PMID: 18006307
Bioisosteric replacements of the pyrazole moiety of rimonabant: synthesis, biological properties, and molecular modeling investigations of thiazoles, triazoles, and imidazoles as potent and selective CB1 cannabinoid receptor antagonists.
Lange JH, van Stuivenberg HH, Coolen HK, Adolfs TJ, McCreary AC, Keizer HG, Wals HC, Veerman W, Borst AJ, de Looff W, Verveer PC, Kruse CG. Lange JH, et al. Among authors: keizer hg. J Med Chem. 2005 Mar 24;48(6):1823-38. doi: 10.1021/jm040843r. J Med Chem. 2005. PMID: 15771428
Synthesis, structure-activity relationships, and biological properties of 1-heteroaryl-4-[omega-(1H-indol-3-yl)alkyl]piperazines, novel potential antipsychotics combining potent dopamine D2 receptor antagonism with potent serotonin reuptake inhibition.
Smid P, Coolen HK, Keizer HG, van Hes R, de Moes JP, den Hartog AP, Stork B, Plekkenpol RH, Niemann LC, Stroomer CN, Tulp MT, van Stuivenberg HH, McCreary AC, Hesselink MB, Herremans AH, Kruse CG. Smid P, et al. Among authors: keizer hg. J Med Chem. 2005 Nov 3;48(22):6855-69. doi: 10.1021/jm050148z. J Med Chem. 2005. PMID: 16250644
N'-(arylsulfonyl)pyrazoline-1-carboxamidines as novel, neutral 5-hydroxytryptamine 6 receptor (5-HT₆R) antagonists with unique structural features.
van Loevezijn A, Venhorst J, Iwema Bakker WI, de Korte CG, de Looff W, Verhoog S, van Wees JW, van Hoeve M, van de Woestijne RP, van der Neut MA, Borst AJ, van Dongen MJ, de Bruin NM, Keizer HG, Kruse CG. van Loevezijn A, et al. Among authors: keizer hg. J Med Chem. 2011 Oct 27;54(20):7030-54. doi: 10.1021/jm200466r. Epub 2011 Sep 26. J Med Chem. 2011. PMID: 21866910
Changes in subcellular doxorubicin distribution and cellular accumulation alone can largely account for doxorubicin resistance in SW-1573 lung cancer and MCF-7 breast cancer multidrug resistant tumour cells.
Schuurhuis GJ, van Heijningen TH, Cervantes A, Pinedo HM, de Lange JH, Keizer HG, Broxterman HJ, Baak JP, Lankelma J. Schuurhuis GJ, et al. Among authors: keizer hg. Br J Cancer. 1993 Nov;68(5):898-908. doi: 10.1038/bjc.1993.452. Br J Cancer. 1993. PMID: 8105865 Free PMC article.
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