Synthesis of 131I-Labeled Glucose-Conjugated Inhibitors of O 6-Methylguanine-DNA Methyltransferase (MGMT) and Comparison with Nonconjugated Inhibitors as …

…, B Lecher, M Briegert, A Piee-Staffa…

Index: Muehlhausen, Ute; Schirrmacher, Ralf; Piel, Markus; Lecher, Bernd; Briegert, Manuela; Piee-Staffa, Andrea; Kaina, Bernd; Roesch, Frank Journal of Medicinal Chemistry, 2006 , vol. 49, # 1 p. 263 - 272

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Citation Number: 20

Abstract

O 6-Substituted guanine derivatives are powerful agents used for tumor cell sensitization by inhibition of the DNA repair enzyme O 6-methylguanine-DNA methyltransferase (MGMT). To provide targeted accumulation of MGMT inhibitors in tumor tissue as well as tools for in vivo imaging, we synthesized iodinated C8-alkyl-linked glucose conjugates of 2-amino-6-(5- iodothenyl)-9 H-purine (O 6-(5-iodothenyl) guanine, ITG) and 2-amino-6-(3-iodobenzyloxy ...