In view of the property of porphyrin＇s accumulation selectively in tumor, the ftorafur was modified by binding a porphyrin block to improve its tumor targeting and reduce its side effects. These novel porphyrin deriv...In view of the property of porphyrin＇s accumulation selectively in tumor, the ftorafur was modified by binding a porphyrin block to improve its tumor targeting and reduce its side effects. These novel porphyrin derivatives and metal compounds were synthesized under mild conditions with satisfactory yield, and the constructions of all these new compounds were characterized by UV, IR, MS, ^1H NMR spectra and elementary analysis. Their anticancer activities were evaluated by MTT assay; the results indicated that the anticancer activities of compounds 4a-e were twice as high as that of ftorafur.展开更多
A novel series of quaternary ammonium cationic derivatives based on tetrapyridyl-porphyrin was synthesized. All the compounds were evaluated for their in vitro antibacterial activities against S. aureus, E. coli and P...A novel series of quaternary ammonium cationic derivatives based on tetrapyridyl-porphyrin was synthesized. All the compounds were evaluated for their in vitro antibacterial activities against S. aureus, E. coli and P. aeruginosa, and antifungal activities against C. albicans, where microorganisms were exposed and unexposed to the irradiation. The results revealed that some of these compounds, especially, 3a and 4a displayed satisfactory antibacterial activity against Gram-positive bacteria S. aureus and moderate antifungal activity against C. albicans. Unfortunately, Gram-negative bacteria P aeruginasa was resistant to all compounds. The antimicrobial activity was found to be sensitive to the functional groups attached on the aromatic ring and the complex metal in the porphyrin ring, and decreased with the increase of electron-withdrawing capability of the functional groups. These preliminary results suggested that the remarkable antibacterial efficiency against S. aureus makes these substances promising antimicrobial agents.展开更多
文摘In view of the property of porphyrin＇s accumulation selectively in tumor, the ftorafur was modified by binding a porphyrin block to improve its tumor targeting and reduce its side effects. These novel porphyrin derivatives and metal compounds were synthesized under mild conditions with satisfactory yield, and the constructions of all these new compounds were characterized by UV, IR, MS, ^1H NMR spectra and elementary analysis. Their anticancer activities were evaluated by MTT assay; the results indicated that the anticancer activities of compounds 4a-e were twice as high as that of ftorafur.
基金the School of Pharmacy of Southwest University for their partial support to this work.
文摘A novel series of quaternary ammonium cationic derivatives based on tetrapyridyl-porphyrin was synthesized. All the compounds were evaluated for their in vitro antibacterial activities against S. aureus, E. coli and P. aeruginosa, and antifungal activities against C. albicans, where microorganisms were exposed and unexposed to the irradiation. The results revealed that some of these compounds, especially, 3a and 4a displayed satisfactory antibacterial activity against Gram-positive bacteria S. aureus and moderate antifungal activity against C. albicans. Unfortunately, Gram-negative bacteria P aeruginasa was resistant to all compounds. The antimicrobial activity was found to be sensitive to the functional groups attached on the aromatic ring and the complex metal in the porphyrin ring, and decreased with the increase of electron-withdrawing capability of the functional groups. These preliminary results suggested that the remarkable antibacterial efficiency against S. aureus makes these substances promising antimicrobial agents.
