3-喹啉/3-吡啶混合取代阳离子型卟啉化合物的制备和生物活性研究
Preparation and Bioactivity of Cationic Porphyrins Bearing Mixed 3-quinolyl and 3-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: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。Abstract: To search for the poten t te lomerase inhibitors with structures of cationic porphyrins to improve the intera ctions between G q uadruplex and porphyrins by systematically varying the meso substituents. Porphyrins bearing mixed 3 quinolyl/3 pyridyl mes