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
A visible light-promoted fast photochemical Wolff rearrangement was developed toward synthesis ofα-substituted amides in continuous flow with the use of a photochemical oscillatory flow reactor(POFR).The control expe...A visible light-promoted fast photochemical Wolff rearrangement was developed toward synthesis ofα-substituted amides in continuous flow with the use of a photochemical oscillatory flow reactor(POFR).The control experiment indicates that a fast process of the Wolff rearrangement(<40 s)is involved.Notably,this protocol does not require excess use of any reactants,and the resultingα-substituted amides could be isolated by recrystallization in good to excellent yields.展开更多
目的探讨肠道屏障功能、IL-6、血沉(erythrocyte sedimentation rate,ESR)指标在克罗恩病合并贫血患者中的变化及应用价值。方法选取2022年6月至2023年4月至南京市第二医院就诊的克罗恩病患者155例。根据血红蛋白检测结果将患者分为贫血...目的探讨肠道屏障功能、IL-6、血沉(erythrocyte sedimentation rate,ESR)指标在克罗恩病合并贫血患者中的变化及应用价值。方法选取2022年6月至2023年4月至南京市第二医院就诊的克罗恩病患者155例。根据血红蛋白检测结果将患者分为贫血组(55例)及非贫血组(100例),对两组间DAO、D-LA、BT、IL-6及ESR水平进行比较,并进行相关统计学分析。结果与非贫血组相比,贫血组患者D-LA水平明显降低,IL-6及ESR水平显著升高,差异有统计学意义(P<0.05),两组间DAO、BT水平差异无统计学意义(P>0.05);在贫血组中,血清D-LA水平与BT水平呈正相关、与IL-6呈负相关;二元Logistic回归分析结果显示,ESR水平是克罗恩病患者贫血的独立影响因素(OR=1.963,P<0.05);D-LA、IL-6及ESR判断克罗恩病合并贫血的ROC曲线下面积(area under the curve,AUC)分别为0.322、0.714、0.737(P均<0.05),DAO及BT的AUC差异无统计学意义。结论克罗恩病合并贫血患者肠道屏障功能、IL-6及ESR水平发生明显变化,做好其分析对克罗恩病患者的贫血发生机制研究以及临床诊疗具有积极意义。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.
基金financial support from the National Natural Science Foundation of China(No.22208279)Financial support from the Fuzhou University(No.0041/511095)。
文摘A visible light-promoted fast photochemical Wolff rearrangement was developed toward synthesis ofα-substituted amides in continuous flow with the use of a photochemical oscillatory flow reactor(POFR).The control experiment indicates that a fast process of the Wolff rearrangement(<40 s)is involved.Notably,this protocol does not require excess use of any reactants,and the resultingα-substituted amides could be isolated by recrystallization in good to excellent yields.
文摘目的探讨肠道屏障功能、IL-6、血沉(erythrocyte sedimentation rate,ESR)指标在克罗恩病合并贫血患者中的变化及应用价值。方法选取2022年6月至2023年4月至南京市第二医院就诊的克罗恩病患者155例。根据血红蛋白检测结果将患者分为贫血组(55例)及非贫血组(100例),对两组间DAO、D-LA、BT、IL-6及ESR水平进行比较,并进行相关统计学分析。结果与非贫血组相比,贫血组患者D-LA水平明显降低,IL-6及ESR水平显著升高,差异有统计学意义(P<0.05),两组间DAO、BT水平差异无统计学意义(P>0.05);在贫血组中,血清D-LA水平与BT水平呈正相关、与IL-6呈负相关;二元Logistic回归分析结果显示,ESR水平是克罗恩病患者贫血的独立影响因素(OR=1.963,P<0.05);D-LA、IL-6及ESR判断克罗恩病合并贫血的ROC曲线下面积(area under the curve,AUC)分别为0.322、0.714、0.737(P均<0.05),DAO及BT的AUC差异无统计学意义。结论克罗恩病合并贫血患者肠道屏障功能、IL-6及ESR水平发生明显变化,做好其分析对克罗恩病患者的贫血发生机制研究以及临床诊疗具有积极意义。
