6-Substituted 5,8-O-dimethyl-1,4-naphthoquinones（6-DMNQ）,the promising anticancer scaffolds,were selectively generated by oxidative demethylation of 2-substituted 1,4,5,8-tetramethoxynaphthalenes with CAN in EtOAc/H...6-Substituted 5,8-O-dimethyl-1,4-naphthoquinones（6-DMNQ）,the promising anticancer scaffolds,were selectively generated by oxidative demethylation of 2-substituted 1,4,5,8-tetramethoxynaphthalenes with CAN in EtOAc/H2O in comparatively high yields.An interesting finding was that apart from the reported electron-withdrawing effects of substituents on position 2 of naphthalene ring,regioselective synthesis of 6-DMNQ was largely dependent on the steric effects in CAN-mediated oxidation.The selective cytotoxicities of 6-DMNQ from the in vitro cell-based assays were exhibited between the cancer cells and normal cells.Moreover,most of sulfur-containing 6-DMNQ derivatives displayed better anticancer activities than the corresponding oxygen-containing ones,which could provide an available strategy for the design of 6-DMNQ derivatives as potential anticancer agents.展开更多
Fifteen 1-（4-substituted phenyl）-4-（4-bromophenyl）-5-（halo-o-hydroxyphenyl）imino-1,2,3-triazoles were designed and synthe- sized based on rational combination of 1,2,3-triazoles and （halo）o-hydroxyphenyl group...Fifteen 1-（4-substituted phenyl）-4-（4-bromophenyl）-5-（halo-o-hydroxyphenyl）imino-1,2,3-triazoles were designed and synthe- sized based on rational combination of 1,2,3-triazoles and （halo）o-hydroxyphenyl group according to the superposition principle of reinforcement of biological activities. All the compounds were tested to an in vitro antimicrobial screening against M.a. and E.c.. Compounds IIe-IIo exhibited more potent antimicrobial activities against M.a. and E.c. than triclosan and fluconazole, which provided valuable information to further study of novel antimicrobial research.展开更多
基金supported by National Natural Science Foundation of China(No.81373274)Ph.D.Programs Foundation of Ministry of Education China(No.20120073110068)Shanghai Biomedical Supporting Funding(No.15431900600)
文摘6-Substituted 5,8-O-dimethyl-1,4-naphthoquinones（6-DMNQ）,the promising anticancer scaffolds,were selectively generated by oxidative demethylation of 2-substituted 1,4,5,8-tetramethoxynaphthalenes with CAN in EtOAc/H2O in comparatively high yields.An interesting finding was that apart from the reported electron-withdrawing effects of substituents on position 2 of naphthalene ring,regioselective synthesis of 6-DMNQ was largely dependent on the steric effects in CAN-mediated oxidation.The selective cytotoxicities of 6-DMNQ from the in vitro cell-based assays were exhibited between the cancer cells and normal cells.Moreover,most of sulfur-containing 6-DMNQ derivatives displayed better anticancer activities than the corresponding oxygen-containing ones,which could provide an available strategy for the design of 6-DMNQ derivatives as potential anticancer agents.
基金supported by the National Natural Science Foundation of China (No. 20976135)
文摘Fifteen 1-（4-substituted phenyl）-4-（4-bromophenyl）-5-（halo-o-hydroxyphenyl）imino-1,2,3-triazoles were designed and synthe- sized based on rational combination of 1,2,3-triazoles and （halo）o-hydroxyphenyl group according to the superposition principle of reinforcement of biological activities. All the compounds were tested to an in vitro antimicrobial screening against M.a. and E.c.. Compounds IIe-IIo exhibited more potent antimicrobial activities against M.a. and E.c. than triclosan and fluconazole, which provided valuable information to further study of novel antimicrobial research.
