中国药科大学学报2003，Vol.34Issue(2)：109-115,7.
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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作者信息
- 1. College of Pharmacy and Arizona Cancer Center, University of Arizona, Tucson AZ85742,USA;College of Pharmacy and Arizona Cancer Center, University of Arizona, Tucson AZ85742,USA;College of Pharmacy and Arizona Cancer Center, University of Arizona, Tucson AZ85742,USA;College of Pharmacy and Arizona Cancer Center, University of Arizona, Tucson AZ85742,USA;College of Pharmacy and Arizona Cancer Center, University of Arizona, Tucson AZ85742,USA
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摘要
Abstract
AIM: To search for the potent telomerase inhibitors with structures of cationic porphyrins to improve the interactions between G-quadruplex and porphyrins by systematically varying the meso substituents. METHOD: Porphyrins bearing mixed 3-quinolyl/3-pyridyl meso groups were synthesized using the Adler-Longo method by condensation of aldehydes with pyrrole, followed by methylation and ion-exchange. The compounds were tested for the telomerase inhibitory activity and c-Myc inhibitory activity. RESULT: All compounds were found to be potent and approximately equivalent in terms of their ability to inhibit the action of telomerase in a cell-free assay. Compound 4 had the best inhibitory activity on c-Myc.关键词
端粒酶/端粒酶抑制剂/G-四链体/卟啉/c-Myc抑制活性/制备Key words
Telomerase/Telomerase inhibitors/G-quadruplex/Porphyrin/c-Myc inhibitory activity分类
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..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[J].中国药科大学学报,2003,34(2):109-115,7.
