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合成一系列O6-苄基鸟嘌呤(O6-BG)类似物,并且采用MTT法评价其体外对DNA修复蛋白AGT的抑制作用,探讨其作为潜在的正电子发射断层成像技术(PET)显像剂前体的可能性。以鸟嘌呤作为起始原料分别合成了O6-BG及其类似物HMBG,MOBG,MOMOBG,BABP和PEG。采用MTT方法,通过测定合成产物增强HeLa细胞对1,3-双(2-氯乙基)亚硝基脲(BCNU)药物敏感性的强弱来评价其对AGT的抑制作用。合成产物对AGT抑制活性强弱排序为HMBG≥O6-BG≥MOBG≥MOMBG,而BABP和PEG基本未表现出任何的AGT抑制活性。HMBG,MOBG和MOMBG具有良好的体外活性,其正电子核素标记物可能成为有前景的用于肿瘤AGT显像的PET显像剂。
A series of O6-benzylguanine (O6-BG) analogs were synthesized and their in vitro inhibitory effect on DNA repair protein AGT was evaluated by MTT assay as a potential PET imaging agent Precursor possibilities. O6-BG and its analogues HMBG, MOBG, MOMOBG, BABP and PEG were synthesized using guanine as a starting material. MTT assay was used to evaluate the inhibitory effect of the synthesized products on the sensitivity of HeLa cells to 1, 3-bis (2-chloroethyl) nitrosourea (BCNU). The order of the inhibitory activity of the synthesized products against AGT was HMBG ≧ O6-BG ≧ MOBG ≧ MOMBG, while the BABP and PEG did not show any AGT inhibitory activity. HMBG, MOBG and MOMBG have good in vitro activity and positron-nuclide markers may become promising PET imaging agents for tumor AGT imaging.