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New tetrahydroisoquinoline-based P-glycoprotein modulators: decoration of the biphenyl core gives selective ligands.
Contino M, Guglielmo S, Perrone MG, Giampietro R, Rolando B, Carrieri A, Zaccaria D, Chegaev K, Borio V, Riganti C, Zabielska-Koczywąs K, Colabufo NA, Fruttero R. Contino M, et al. Among authors: giampietro r. Medchemcomm. 2018 Apr 3;9(5):862-869. doi: 10.1039/c8md00075a. eCollection 2018 May 1. Medchemcomm. 2018. PMID: 30108975 Free PMC article.
Design, Biological Evaluation, and Molecular Modeling of Tetrahydroisoquinoline Derivatives: Discovery of A Potent P-Glycoprotein Ligand Overcoming Multidrug Resistance in Cancer Stem Cells.
Riganti C, Contino M, Guglielmo S, Perrone MG, Salaroglio IC, Milosevic V, Giampietro R, Leonetti F, Rolando B, Lazzarato L, Colabufo NA, Fruttero R. Riganti C, et al. Among authors: giampietro r. J Med Chem. 2019 Jan 24;62(2):974-986. doi: 10.1021/acs.jmedchem.8b01655. Epub 2019 Jan 9. J Med Chem. 2019. PMID: 30584838 Free article.
One molecule two goals: A selective P-glycoprotein modulator increases drug transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells.
Contino M, Guglielmo S, Riganti C, Antonello G, Perrone MG, Giampietro R, Rolando B, Fruttero R, Colabufo NA. Contino M, et al. Among authors: giampietro r. Eur J Med Chem. 2020 Dec 15;208:112843. doi: 10.1016/j.ejmech.2020.112843. Epub 2020 Sep 17. Eur J Med Chem. 2020. PMID: 33007664 Free article.
6,7-Dimethoxy-2-phenethyl-1,2,3,4-tetrahydroisoquinoline amides and corresponding ester isosteres as multidrug resistance reversers.
Braconi L, Bartolucci G, Contino M, Chiaramonte N, Giampietro R, Manetti D, Perrone MG, Romanelli MN, Colabufo NA, Riganti C, Dei S, Teodori E. Braconi L, et al. Among authors: giampietro r. J Enzyme Inhib Med Chem. 2020 Dec;35(1):974-992. doi: 10.1080/14756366.2020.1747449. J Enzyme Inhib Med Chem. 2020. PMID: 32253945 Free PMC article.
Design and synthesis of fluorescent ligands for the detection of cannabinoid type 2 receptor (CB2R).
Spinelli F, Giampietro R, Stefanachi A, Riganti C, Kopecka J, Abatematteo FS, Leonetti F, Colabufo NA, Mangiatordi GF, Nicolotti O, Perrone MG, Brea J, Loza MI, Infantino V, Abate C, Contino M. Spinelli F, et al. Among authors: giampietro r. Eur J Med Chem. 2020 Feb 15;188:112037. doi: 10.1016/j.ejmech.2020.112037. Epub 2020 Jan 7. Eur J Med Chem. 2020. PMID: 31954990 Free article.
Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers.
Teodori E, Contino M, Riganti C, Bartolucci G, Braconi L, Manetti D, Romanelli MN, Trezza A, Athanasios A, Spiga O, Perrone MG, Giampietro R, Gazzano E, Salerno M, Colabufo NA, Dei S. Teodori E, et al. Among authors: giampietro r. Eur J Med Chem. 2019 Nov 15;182:111655. doi: 10.1016/j.ejmech.2019.111655. Epub 2019 Aug 30. Eur J Med Chem. 2019. PMID: 31494468
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