1.Preparation and Bioactivity of Cationic Porphyrins Bearing Mixed 3-quinolyl and 3-pyridyl Meso Groups
Lu TAO ; Shi DONGFANG ; Sun DAEKYU ; Han HAIYONG ; H.hurley LAURENCE
Journal of China Pharmaceutical University 2003;(2):109-115
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.
2.Design,Synthesis and Biological Activity of Cationic Porphyrins Bearing Mixed 3-Quinolyl and 4-Pyridyl Meso Groups
Tao LU ; Dongfang SHI ; Daekyu SUN ; Haiyong HAN ; H.hurley LAURENCE
Journal of China Pharmaceutical University 2005;(5):393-397
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.