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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/4-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。结论:阳离子型卟啉化合物是潜在的抗肿瘤候选化合物。
Objective: To find a potent telomerase inhibitor with cationic porphyrin structure. Methods: Various combinations of 3-quinoline / 4-pyridylporphyrin bases were obtained by the condensation reaction of aromatic aldehydes and pyrroles by Adler-Longo porphyrin synthesis method, and then methylated and ion-exchanged to obtain cationic porphyrin The compound. The synthesized compounds were tested for telomerase inhibitory activity and c-Myc inhibitory activity. Results: Acellular experiments show that the synthesized compounds have strong telomerase inhibitory activity, while compound 4 shows the strongest c-Myc inhibitory activity. Conclusion: Cationic porphyrin compounds are potential anti-tumor candidate compounds.