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目的 :寻找具有阳离子型卟啉结构的强效端粒酶抑制剂。方法 :通过芳香醛和吡咯的缩合反应制得 4 乙酰氨基苯基或 4 乙酰氨基苯基 / 4 吡啶基卟啉 ,经水解得相应氨基物 ,然后采用Skraup喹啉合成法制备 6 喹啉 / 4 吡啶取代卟啉碱基 ,最后经甲基化、离子交换得阳离子型卟啉化合物。同法制得 6 喹啉 / 3喹啉 取代卟啉碱基。测试所合成化合物的端粒酶抑制活性。结果 :非细胞试验显示所合成的化合物具有强的端粒酶抑制活性
Objective: To find a potent telomerase inhibitor with cationic porphyrin structure. Methods: 4-Acetamidophenyl or 4-acetylaminophenyl / 4-pyridylporphyrin was prepared through the condensation reaction of aromatic aldehyde and pyrrole. The corresponding amino group was hydrolyzed to obtain 6quinoline / 4 Pyridine substituted porphyrin base, the final methylation, ion exchange cationic porphyrin compounds. With the legal system 6 quinoline / 3 quinoline substituted porphyrin base. The synthesized compounds were tested for their telomerase inhibitory activity. Results: Acellular experiments showed that the synthesized compounds have strong telomerase inhibitory activity