喹啉或喹啉/吡啶混合取代阳离子型卟啉化合物的制备和端粒酶抑制活性研究
Preparation and Telomerase Inhibition of Cationic Porphyrins Bearing Quinolyl and Mixed Quinolyl/pyridyl Meso Groups
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摘要: 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、离子交换得是离子型卟啉化合物,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。Abstract: AIM\ The purpose is to search for the potent telomerase inhibitors with structures of cationic porphyrins. METHODS\ Porphyrins bearing 6 quinolyl and mixed 6 quinolyl/4 pyridyl meso groups were synthesized using Skraup quinoline methodology from porphy