Marquage par ¹⁴C ET ¹³C de la N acetyl O₆ benzyl guanosine

Abstract

O6 Benzyl N acetyl guanosine a new inhibitor of O6 Alkyl Guanine transferase (O6AGT) was labelled by 14C and 13C on the benzyl methylen group in order to realize a pharmacokinetic study on nude mice grafted with human tumors. The labelling yield calculated from the precursor (Ba 14 or 13CO3) is in the range of 15%.

Circadian variation inO6-alkylguanine-DNA alkyltransferase activity in circulating blood mononuclear cells of healthy human subjects

“…25,26 Cells were disrupted by sonication in 100 l/10 7 cells of lysis buffer (70 mM N-2-hydroxyethyl-piperazine-NЈ-2-ethanolsulfonic acid, pH 7.8; 1 mM EDTA; 1 mM dithiothreitol; 400 mM NaCl; 10% glycerol; 1 g/ml leupeptine-antipain-aprotinine) 3 times for 45 sec each at 1 min intervals on ice. 28 Supernatants were kept at Ϫ80°C after measurement of total protein concentration using the Bradford method with bovine serum albumin as standard.…”

Synthetic Strategies Towards O6-Substituted Guanine Derivatives and their Application in Medicine

“…These compounds have been suggested for imaging breast cancer with PET and were also displayed elsewhere [40]. It should also be mentioned that different groups introduced tritium [41,42], carbon-14 [43], phosphorus-32 [44] and sulfur-35 [45] into O 6 -substituted guanine derivatives for measuring the AGT activity.…”

O6-3-[131I]iodobenzylguanine: Improved Synthesis and Further Evaluation of a Potential Agent for Imaging of Alkylguanine-DNA Alkyltransferase

“…With regard to currently available potential radiolabeled AGT probes, the preparation of 125 I-labeled guanosine derivatives has been reported but their usefulness as an AGT labeling agents was not evaluated (9). A 14 Clabeled guanosine derivative (10) and a BG derivative labeled with 3 H (11) also have been described; however, it is not practical to perform external imaging of these radionuclides. More recently, the synthesis of several BG derivatives labeled with 11 C and 18 F have been reported but the in vivo behavior of these tracers has largely been unexplored (12)(13)(14)(15)(16)(17).…”