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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: gregson sj. 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
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: gregson sj. 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.
Pyrrolobenzodiazepine Dimer Antibody-Drug Conjugates: Synthesis and Evaluation of Noncleavable Drug-Linkers.
Gregson SJ, Masterson LA, Wei B, Pillow TH, Spencer SD, Kang GD, Yu SF, Raab H, Lau J, Li G, Lewis Phillips GD, Gunzner-Toste J, Safina BS, Ohri R, Darwish M, Kozak KR, Dela Cruz-Chuh J, Polson A, Flygare JA, Howard PW. Gregson SJ, et al. J Med Chem. 2017 Dec 14;60(23):9490-9507. doi: 10.1021/acs.jmedchem.7b00736. Epub 2017 Nov 16. J Med Chem. 2017. PMID: 29112410
95 results