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Discovery of DB18, a potent inhibitor of CLK kinases with a high selectivity against DYRK1A kinase.
Brahmaiah D, Kanaka Durga Bhavani A, Aparna P, Sampath Kumar N, Solhi H, Le Guevel R, Baratte B, Ruchaud S, Bach S, Singh Jadav S, Raji Reddy C, Roisnel T, Mosset P, Levoin N, Grée R. Brahmaiah D, et al. Among authors: le guevel r. Bioorg Med Chem. 2021 Feb 1;31:115962. doi: 10.1016/j.bmc.2020.115962. Epub 2020 Dec 31. Bioorg Med Chem. 2021. PMID: 33422908
Synthesis and biological studies of new piperidino-1,2,3-triazole hybrids with 3-aryl isoxazole side chains.
Murthy AVR, Narendar V, Sampath Kumar N, Aparna P, Bhavani AKD, Solhi H, Le Guevel R, Roul J, Gautier F, Juin P, Reddy CR, Mosset P, Levoin N, Grée R. Murthy AVR, et al. Among authors: le guevel r. Bioorg Med Chem Lett. 2021 Nov 15;52:128390. doi: 10.1016/j.bmcl.2021.128390. Epub 2021 Sep 30. Bioorg Med Chem Lett. 2021. PMID: 34601029 Free article.
Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3.
Oukoloff K, Coquelle N, Bartolini M, Naldi M, Le Guevel R, Bach S, Josselin B, Ruchaud S, Catto M, Pisani L, Denora N, Iacobazzi RM, Silman I, Sussman JL, Buron F, Colletier JP, Jean L, Routier S, Renard PY. Oukoloff K, et al. Among authors: le guevel r. Eur J Med Chem. 2019 Apr 15;168:58-77. doi: 10.1016/j.ejmech.2018.12.063. Epub 2019 Feb 13. Eur J Med Chem. 2019. PMID: 30798053 Free article.
Functionalization of 9-thioxanthone at the 1-position: From arylamino derivatives to [1]benzo(thio)pyrano[4,3,2-de]benzothieno[2,3-b]quinolines of biological interest.
Mokhtari Brikci-Nigassa N, Nauton L, Moreau P, Mongin O, Duval RE, Picot L, Thiéry V, Souab M, Baratte B, Ruchaud S, Bach S, Le Guevel R, Bentabed-Ababsa G, Erb W, Roisnel T, Dorcet V, Mongin F. Mokhtari Brikci-Nigassa N, et al. Among authors: le guevel r. Bioorg Chem. 2020 Jan;94:103347. doi: 10.1016/j.bioorg.2019.103347. Epub 2019 Oct 10. Bioorg Chem. 2020. PMID: 31810757
Novel optimization of valmerins (tetrahydropyrido[1,2-a]isoindolones) as potent dual CDK5/GSK3 inhibitors.
Ouach A, Boulahjar R, Vala C, Bourg S, Bonnet P, Guguen-Guillouzo C, Ravache M, Le Guevel R, Lozach O, Lazar S, Troin Y, Meijer L, Ruchaud S, Akssira M, Guillaumet G, Routier S. Ouach A, et al. Among authors: le guevel r. Eur J Med Chem. 2016 Jun 10;115:311-25. doi: 10.1016/j.ejmech.2016.02.072. Epub 2016 Mar 2. Eur J Med Chem. 2016. PMID: 27019296
Advances in tetrahydropyrido[1,2-a]isoindolone (valmerins) series: Potent glycogen synthase kinase 3 and cyclin dependent kinase 5 inhibitors.
Boulahjar R, Ouach A, Bourg S, Bonnet P, Lozach O, Meijer L, Guguen-Guillouzo C, Le Guevel R, Lazar S, Akssira M, Troin Y, Guillaumet G, Routier S. Boulahjar R, et al. Among authors: le guevel r. Eur J Med Chem. 2015 Aug 28;101:274-87. doi: 10.1016/j.ejmech.2015.06.046. Epub 2015 Jun 27. Eur J Med Chem. 2015. PMID: 26142492 Free article.
Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
Oger F, Lecorgne A, Sala E, Nardese V, Demay F, Chevance S, Desravines DC, Aleksandrova N, Le Guével R, Lorenzi S, Beccari AR, Barath P, Hart DJ, Bondon A, Carettoni D, Simonneaux G, Salbert G. Oger F, et al. Among authors: le guevel r. J Med Chem. 2010 Mar 11;53(5):1937-50. doi: 10.1021/jm901561u. J Med Chem. 2010. PMID: 20143840
47 results