Preparation and Bioactivity of Cationic Porphyrins Bearing Mixed 3-quinolyl and 3-pyridyl Meso Groups
- VernacularTitle: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
- Author:
Lu TAO
;
Shi DONGFANG
;
Sun DAEKYU
;
Han HAIYONG
;
H.hurley LAURENCE
- Publication Type:Journal Article
- Keywords:
Telomerase;
Telomerase inhibitors;
G-quadruplex;
Porphyrin;
c-Myc inhibitory activity
- From:
Journal of China Pharmaceutical University
2003;(2):109-115
- 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. 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.
