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Synthesis of a novel C2/C2'-aryl-substituted pyrrolo[2,1-c][1,4]benzodiazepine dimer prodrug with improved water solubility and reduced DNA reaction rate.
Howard PW, Chen Z, Gregson SJ, Masterson LA, Tiberghien AC, Cooper N, Fang M, Coffils MJ, Klee S, Hartley JA, Thurston DE. Howard PW, et al. Among authors: tiberghien ac. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6463-6. doi: 10.1016/j.bmcl.2009.09.012. Epub 2009 Sep 9. Bioorg Med Chem Lett. 2009. PMID: 19811912
Structure-activity relationships of monomeric C2-aryl pyrrolo[2,1-c][1,4]benzodiazepine (PBD) antitumor agents.
Antonow D, Kaliszczak M, Kang GD, Coffils M, Tiberghien AC, Cooper N, Barata T, Heidelberger S, James CH, Zloh M, Jenkins TC, Reszka AP, Neidle S, Guichard SM, Jodrell DI, Hartley JA, Howard PW, Thurston DE. Antonow D, et al. Among authors: tiberghien ac. J Med Chem. 2010 Apr 8;53(7):2927-41. doi: 10.1021/jm901722v. J Med Chem. 2010. PMID: 20218628
SG2285, a novel C2-aryl-substituted pyrrolobenzodiazepine dimer prodrug that cross-links DNA and exerts highly potent antitumor activity.
Hartley JA, Hamaguchi A, Coffils M, Martin CR, Suggitt M, Chen Z, Gregson SJ, Masterson LA, Tiberghien AC, Hartley JM, Pepper C, Lin TT, Fegan C, Thurston DE, Howard PW. Hartley JA, et al. Among authors: tiberghien ac. Cancer Res. 2010 Sep 1;70(17):6849-58. doi: 10.1158/0008-5472.CAN-10-0790. Epub 2010 Jul 26. Cancer Res. 2010. PMID: 20660714 Free PMC article.
A potent anti-CD70 antibody-drug conjugate combining a dimeric pyrrolobenzodiazepine drug with site-specific conjugation technology.
Jeffrey SC, Burke PJ, Lyon RP, Meyer DW, Sussman D, Anderson M, Hunter JH, Leiske CI, Miyamoto JB, Nicholas ND, Okeley NM, Sanderson RJ, Stone IJ, Zeng W, Gregson SJ, Masterson L, Tiberghien AC, Howard PW, Thurston DE, Law CL, Senter PD. Jeffrey SC, et al. Bioconjug Chem. 2013 Jul 17;24(7):1256-63. doi: 10.1021/bc400217g. Epub 2013 Jun 28. Bioconjug Chem. 2013. PMID: 23808985
Genetically Encoded Azide Containing Amino Acid in Mammalian Cells Enables Site-Specific Antibody-Drug Conjugates Using Click Cycloaddition Chemistry.
VanBrunt MP, Shanebeck K, Caldwell Z, Johnson J, Thompson P, Martin T, Dong H, Li G, Xu H, D'Hooge F, Masterson L, Bariola P, Tiberghien A, Ezeadi E, Williams DG, Hartley JA, Howard PW, Grabstein KH, Bowen MA, Marelli M. VanBrunt MP, et al. Among authors: tiberghien a. Bioconjug Chem. 2015 Nov 18;26(11):2249-60. doi: 10.1021/acs.bioconjchem.5b00359. Epub 2015 Sep 11. Bioconjug Chem. 2015. PMID: 26332743
ADCT-301, a Pyrrolobenzodiazepine (PBD) Dimer-Containing Antibody-Drug Conjugate (ADC) Targeting CD25-Expressing Hematological Malignancies.
Flynn MJ, Zammarchi F, Tyrer PC, Akarca AU, Janghra N, Britten CE, Havenith CE, Levy JN, Tiberghien A, Masterson LA, Barry C, D'Hooge F, Marafioti T, Parren PW, Williams DG, Howard PW, van Berkel PH, Hartley JA. Flynn MJ, et al. Among authors: tiberghien a. Mol Cancer Ther. 2016 Nov;15(11):2709-2721. doi: 10.1158/1535-7163.MCT-16-0233. Epub 2016 Aug 17. Mol Cancer Ther. 2016. PMID: 27535974
35 results