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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 :采用Adler Longo卟啉合成法通过芳香醛和吡咯的缩合反应制得各种组合的 3 喹啉 /3 吡啶基卟啉碱基 ,再经甲基化、离子交换得阳离子型卟啉化合物。测试所合成化合物的端粒酶抑制活性和c Myc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 ;而化合物 4显示最强的c Myc抑制活性。
Objective: To find a potent telomerase inhibitor with cationic porphyrin structure. Methods: Various combinations of 3-quinoline / 3-pyridylporphyrin bases were obtained by the condensation reaction of aromatic aldehyde and pyrrole by Adler Longo porphyrin synthesis method, and then methylated and ion-exchanged to obtain cationic porphyrin compounds. The synthesized compounds were tested for telomerase inhibitory activity and c Myc inhibitory activity. Results: Acellular experiments showed that the synthesized compounds had strong telomerase inhibitory activity, while compound 4 showed the strongest c Myc inhibitory activity.