In an attempt to find new antitumor agents,a novel class of chromone compounds with a benzimidazole or a benzoxazole ring in positions 2 or 6 were synthesized via condensation in polyphosphoric acid(PPA) by using chro...In an attempt to find new antitumor agents,a novel class of chromone compounds with a benzimidazole or a benzoxazole ring in positions 2 or 6 were synthesized via condensation in polyphosphoric acid(PPA) by using chromone acids as the starting materials. During the preparation process,it was found that PPA could cleave the chromone ring to produce a ring-opening compound(6). The molar ratio of the chromone compound(5) to the ring-opening compound(6) varied with the change of reaction temperature and time. Based on MTT protocol,the antitumor activity of each of the compounds obtained was evaluated against three human cancer cell lines: KB(oral epidermal),A2780(ovary) and Bel7402(liver). The IC_ 50 varied from 54.7 μmol/L to more than 180 μmol/L.展开更多
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
目的:分析二肽基肽酶样蛋白-6(dipeptidyl-peptidase-like protein 6,DPPX)抗体相关脑炎患者的临床特征。方法:对2016年1月—2025年2月南京医科大学附属脑科医院就诊的5例DPPX抗体相关脑炎患者的临床特点、脑电图、磁共振成像(magnetic ...目的:分析二肽基肽酶样蛋白-6(dipeptidyl-peptidase-like protein 6,DPPX)抗体相关脑炎患者的临床特征。方法:对2016年1月—2025年2月南京医科大学附属脑科医院就诊的5例DPPX抗体相关脑炎患者的临床特点、脑电图、磁共振成像(magnetic resonance imaging,MRI)及预后进行回顾性研究。结果:5例均为男性,年龄14~56岁。5例患者血清DPPX抗体均为阳性,滴度1∶100~1∶10,其中1例合并血清接触蛋白关联蛋白2(contactin-associated protein-like 2,CASPR2)抗体阳性,4例脑脊液DPPX抗体阴性,1例滴度1∶1。2例患者以行为异常起病,1例以癫痫发作起病,1例以记忆力减退起病,1例合并CASPR2抗体阳性患者以多部位游走性肌阵挛起病。4例患者头颅MRI正常,1例头颅MRI提示双侧颞叶异常信号。以癫痫发作起病的患者脑电图背景重度异常合并左前颞尖波、尖慢波频发。结论:DPPX抗体相关脑炎临床表现具有异质性,早期诊断与鉴别困难,免疫治疗有效,易复发。展开更多
文摘In an attempt to find new antitumor agents,a novel class of chromone compounds with a benzimidazole or a benzoxazole ring in positions 2 or 6 were synthesized via condensation in polyphosphoric acid(PPA) by using chromone acids as the starting materials. During the preparation process,it was found that PPA could cleave the chromone ring to produce a ring-opening compound(6). The molar ratio of the chromone compound(5) to the ring-opening compound(6) varied with the change of reaction temperature and time. Based on MTT protocol,the antitumor activity of each of the compounds obtained was evaluated against three human cancer cell lines: KB(oral epidermal),A2780(ovary) and Bel7402(liver). The IC_ 50 varied from 54.7 μmol/L to more than 180 μmol/L.
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.
