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Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold.
Thum S, Kokornaczyk AK, Seki T, De Maria M, Ortiz Zacarias NV, de Vries H, Weiss C, Koch M, Schepmann D, Kitamura M, Tschammer N, Heitman LH, Junker A, Wünsch B. Thum S, et al. Among authors: de vries h, de maria m. Eur J Med Chem. 2017 Jul 28;135:401-413. doi: 10.1016/j.ejmech.2017.04.046. Epub 2017 Apr 22. Eur J Med Chem. 2017. PMID: 28463783
Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists.
Vilums M, Zweemer AJ, Yu Z, de Vries H, Hillger JM, Wapenaar H, Bollen IA, Barmare F, Gross R, Clemens J, Krenitsky P, Brussee J, Stamos D, Saunders J, Heitman LH, Ijzerman AP. Vilums M, et al. Among authors: de vries h. J Med Chem. 2013 Oct 10;56(19):7706-14. doi: 10.1021/jm4011737. Epub 2013 Sep 27. J Med Chem. 2013. PMID: 24028535
When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists.
Vilums M, Zweemer AJ, Barmare F, van der Gracht AM, Bleeker DC, Yu Z, de Vries H, Gross R, Clemens J, Krenitsky P, Brussee J, Stamos D, Saunders J, Heitman LH, IJzerman AP. Vilums M, et al. Among authors: de vries h. Eur J Med Chem. 2015 Mar 26;93:121-34. doi: 10.1016/j.ejmech.2015.01.063. Epub 2015 Feb 2. Eur J Med Chem. 2015. PMID: 25666912
A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy.
Bot I, Ortiz Zacarías NV, de Witte WE, de Vries H, van Santbrink PJ, van der Velden D, Kröner MJ, van der Berg DJ, Stamos D, de Lange EC, Kuiper J, IJzerman AP, Heitman LH. Bot I, et al. Among authors: de witte we, de vries h, de lange ec. Sci Rep. 2017 Mar 3;7(1):52. doi: 10.1038/s41598-017-00104-z. Sci Rep. 2017. PMID: 28246398 Free PMC article.
1,816 results