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
Two imidazolium bis-estrogens as a new type of biomimetic model, which possesspotential multiple biomimetic functions, were srnthesized in gcod yields by three steps fromestrogen. All new compounds were characterized ...Two imidazolium bis-estrogens as a new type of biomimetic model, which possesspotential multiple biomimetic functions, were srnthesized in gcod yields by three steps fromestrogen. All new compounds were characterized by MS, 1HNMR and elemental analysis.展开更多
A new efficient synthesis of bisphenol A diether bis-imidazoles and bis-benzimidazoles by bromoalkylation and imidazolylation or benzimidazolylation two-step reactions from commercial bisphenol A, imidazole, 2-methyli...A new efficient synthesis of bisphenol A diether bis-imidazoles and bis-benzimidazoles by bromoalkylation and imidazolylation or benzimidazolylation two-step reactions from commercial bisphenol A, imidazole, 2-methylimidazole and benzimidazole is reported.展开更多
The repeat unit of Candida kefyr IFO 0586 strain was designed, and a protected pentasaccharide was synthesized by thirteen-step reactions. Trichloroacetoxy was used as leaving group at anomeric carbon.
the acetate of a novel phenolic glycoside, 1-O-beta-D-glucopyranosyl-( 1-->6)-beta-D-glucopyranosyloxy-3-hydroxy-5-methylbenzene anacardoside, from the fruits of Semecarpus anacardium, and its diastereomer were fir...the acetate of a novel phenolic glycoside, 1-O-beta-D-glucopyranosyl-( 1-->6)-beta-D-glucopyranosyloxy-3-hydroxy-5-methylbenzene anacardoside, from the fruits of Semecarpus anacardium, and its diastereomer were first synthesized using Koenigs-Knorr method from D-glucose through six steps with total yields 33% and 16% respectively.展开更多
A novel one-pot synthesis of 4,5-bis(hydroxymethyl) imidazoles 2a-b, new ethers 3a-b and a new type of imidazolophane 4b by the bis-hydroxymethylation of imidazole or 2-methyl imidazole with formaldehyde and potassium...A novel one-pot synthesis of 4,5-bis(hydroxymethyl) imidazoles 2a-b, new ethers 3a-b and a new type of imidazolophane 4b by the bis-hydroxymethylation of imidazole or 2-methyl imidazole with formaldehyde and potassium hydroxide is reported. The structures of these compounds have been established by MS, (1)HNMR IR and elemental analyses.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.
文摘Two imidazolium bis-estrogens as a new type of biomimetic model, which possesspotential multiple biomimetic functions, were srnthesized in gcod yields by three steps fromestrogen. All new compounds were characterized by MS, 1HNMR and elemental analysis.
文摘A new efficient synthesis of bisphenol A diether bis-imidazoles and bis-benzimidazoles by bromoalkylation and imidazolylation or benzimidazolylation two-step reactions from commercial bisphenol A, imidazole, 2-methylimidazole and benzimidazole is reported.
文摘The repeat unit of Candida kefyr IFO 0586 strain was designed, and a protected pentasaccharide was synthesized by thirteen-step reactions. Trichloroacetoxy was used as leaving group at anomeric carbon.
文摘the acetate of a novel phenolic glycoside, 1-O-beta-D-glucopyranosyl-( 1-->6)-beta-D-glucopyranosyloxy-3-hydroxy-5-methylbenzene anacardoside, from the fruits of Semecarpus anacardium, and its diastereomer were first synthesized using Koenigs-Knorr method from D-glucose through six steps with total yields 33% and 16% respectively.
文摘A novel one-pot synthesis of 4,5-bis(hydroxymethyl) imidazoles 2a-b, new ethers 3a-b and a new type of imidazolophane 4b by the bis-hydroxymethylation of imidazole or 2-methyl imidazole with formaldehyde and potassium hydroxide is reported. The structures of these compounds have been established by MS, (1)HNMR IR and elemental analyses.
