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Structure-Based Optimization of Coumarin hA3 Adenosine Receptor Antagonists.
Matos MJ, Vilar S, Vazquez-Rodriguez S, Kachler S, Klotz KN, Buccioni M, Delogu G, Santana L, Uriarte E, Borges F. Matos MJ, et al. Among authors: kachler s. J Med Chem. 2020 Mar 12;63(5):2577-2587. doi: 10.1021/acs.jmedchem.9b01572. Epub 2019 Dec 4. J Med Chem. 2020. PMID: 31738058
N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice.
Franchetti P, Cappellacci L, Vita P, Petrelli R, Lavecchia A, Kachler S, Klotz KN, Marabese I, Luongo L, Maione S, Grifantini M. Franchetti P, et al. Among authors: kachler s. J Med Chem. 2009 Apr 23;52(8):2393-406. doi: 10.1021/jm801456g. J Med Chem. 2009. PMID: 19317449
Combining selectivity and affinity predictions using an integrated Support Vector Machine (SVM) approach: An alternative tool to discriminate between the human adenosine A(2A) and A(3) receptor pyrazolo-triazolo-pyrimidine antagonists binding sites.
Michielan L, Bolcato C, Federico S, Cacciari B, Bacilieri M, Klotz KN, Kachler S, Pastorin G, Cardin R, Sperduti A, Spalluto G, Moro S. Michielan L, et al. Among authors: kachler s. Bioorg Med Chem. 2009 Jul 15;17(14):5259-74. doi: 10.1016/j.bmc.2009.05.038. Epub 2009 May 21. Bioorg Med Chem. 2009. PMID: 19501513
The significance of 2-furyl ring substitution with a 2-(para-substituted) aryl group in a new series of pyrazolo-triazolo-pyrimidines as potent and highly selective hA(3) adenosine receptors antagonists: new insights into structure-affinity relationship and receptor-antagonist recognition.
Cheong SL, Dolzhenko A, Kachler S, Paoletta S, Federico S, Cacciari B, Dolzhenko A, Klotz KN, Moro S, Spalluto G, Pastorin G. Cheong SL, et al. Among authors: kachler s. J Med Chem. 2010 Apr 22;53(8):3361-75. doi: 10.1021/jm100049f. J Med Chem. 2010. PMID: 20307065
Does the combination of optimal substitutions at the C²-, N⁵- and N⁸-positions of the pyrazolo-triazolo-pyrimidine scaffold guarantee selective modulation of the human A₃ adenosine receptors?
Cheong SL, Dolzhenko AV, Paoletta S, Lee EP, Kachler S, Federico S, Klotz KN, Dolzhenko AV, Spalluto G, Moro S, Pastorin G. Cheong SL, et al. Among authors: kachler s. Bioorg Med Chem. 2011 Oct 15;19(20):6120-34. doi: 10.1016/j.bmc.2011.08.026. Epub 2011 Aug 23. Bioorg Med Chem. 2011. PMID: 21908194
Cytotoxic purine nucleoside analogues bind to A1, A2A, and A3 adenosine receptors.
Jensen K, Johnson LA, Jacobson PA, Kachler S, Kirstein MN, Lamba J, Klotz KN. Jensen K, et al. Among authors: kachler s. Naunyn Schmiedebergs Arch Pharmacol. 2012 May;385(5):519-25. doi: 10.1007/s00210-011-0719-6. Epub 2012 Jan 17. Naunyn Schmiedebergs Arch Pharmacol. 2012. PMID: 22249336 Free PMC article.
49 results