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- W2315262058 abstract "Two radiolabeled analogues of 6-benzyloxy-9H-purin-2-ylamine (O(6)-benzylguanine; BG) potentially useful in the in vivo mapping of O(6)-alkylguanine-DNA alkyltransferase (AGT) were synthesized. Fluorine-18 labeling of the known 6-(4-fluoro-benzyloxy)-9H-purin-2-ylamine (FBG; 6) was accomplished by the condensation of 4-[(18)F]fluorobenzyl alcohol with 2-aminopurin-6-yltrimethylammonium chloride (4) or 2-amino-6-chloropurine in average decay-corrected radiochemical yields of 40 and 25%, respectively. Unlabeled 6-(3-iodo-benzyloxy)-9H-purin-2-ylamine (IBG; 7) was prepared from 4 and 3-iodobenzyl alcohol. Radioiodination of 9, prepared from 7 in two steps, and subsequent deprotection gave [(131)I]7 in about 70% overall radiochemical yield. The IC(50) values for the inactivation of AGT from CHO cells transfected with pCMV-AGT were 15 nM for IBG and 50 nM for FBG. The binding of [(18)F]6 and [(131)I]7 to purified AGT was specific and saturable with both exhibiting similar IC(50) values (5-6 microM)." @default.
- W2315262058 created "2016-06-24" @default.
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- W2315262058 date "2000-10-25" @default.
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- W2315262058 title "Radiolabeled Guanine Derivatives for the in Vivo Mapping of <i>O</i><sup>6</sup>-Alkylguanine-DNA Alkyltransferase: 6-(4-[<sup>18</sup>F]Fluoro-benzyloxy)-9<i>H</i>-purin-2-ylamine and 6-(3-[<sup>131</sup>I]Iodo-benzyloxy)-9<i>H</i>-purin-2-ylamine" @default.
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- W2315262058 doi "https://doi.org/10.1021/bc0000435" @default.
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