Design,Synthesis and Biological Activity of Cationic Porphyrins Bearing Mixed 3-Quinolyl and 4-Pyridyl Meso Groups
- VernacularTitle:3-喹啉/4-吡啶混合取代阳离子型卟啉化合物的设计、合成及其生物活性
- Author:
Tao LU
;
Dongfang SHI
;
Daekyu SUN
;
Haiyong HAN
;
H.hurley LAURENCE
- Publication Type:Journal Article
- Keywords:
Telomerase;
Telomerase inhibitors;
Synthesis;
G-quadruplex;
Porphyrin;
c-Myc inhibitory activity
- From:
Journal of China Pharmaceutical University
2005;(5):393-397
- CountryChina
- Language:Chinese
-
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.METHODS:Porphyrins bearing mixed 3-quinolyl/4-pyridyl meso groups were synthesized using the Adler-Longo method by condensation of aldehydes with pyrrole,and then followed by methylation and ion exchange.The compounds were tested for the telomerase inhibitory activity and c-Myc inhibitory activity.RESULTS: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.CONCLUSION:Cationic porphyrins would be the potential anticancer candidates.
