Robert B. Smith, William Roberts, M. Upenieks, M. Gibson, Michael T. Wentzel, Kyle A. Grice, S. Zingales
Abstract Natural products and their analogs have been explored to stop the progression of cancer cells without unwanted side effects. Chalcones, compounds synthesized naturally in plants, have demonstrated potential as anti-cancer treatments. A library of bis-chalcones that are similar in structure to EF-24, a bis-chalcone molecule known to have anti-cancer properties, has been synthesized in order to examine their medicinal properties. This report highlights the synthesis of ten novel analogs, their anti-cancer activities, and conformational analysis via cryo-NMR and corroboration by density functional theory calculations of the lead compound 1b, tert-butyl 3,5-bis((E)-4-methylbenzylidene)-4-oxopiperidine-1-carboxylate.
{"title":"Synthesis and conformational analysis of N-BOC-protected-3,5-bis(arylidene)-4-piperidone EF-24 analogs as anti-cancer agents","authors":"Robert B. Smith, William Roberts, M. Upenieks, M. Gibson, Michael T. Wentzel, Kyle A. Grice, S. Zingales","doi":"10.1515/hc-2022-0162","DOIUrl":"https://doi.org/10.1515/hc-2022-0162","url":null,"abstract":"Abstract Natural products and their analogs have been explored to stop the progression of cancer cells without unwanted side effects. Chalcones, compounds synthesized naturally in plants, have demonstrated potential as anti-cancer treatments. A library of bis-chalcones that are similar in structure to EF-24, a bis-chalcone molecule known to have anti-cancer properties, has been synthesized in order to examine their medicinal properties. This report highlights the synthesis of ten novel analogs, their anti-cancer activities, and conformational analysis via cryo-NMR and corroboration by density functional theory calculations of the lead compound 1b, tert-butyl 3,5-bis((E)-4-methylbenzylidene)-4-oxopiperidine-1-carboxylate.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":" ","pages":""},"PeriodicalIF":2.3,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48218693","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Xia Yu, Qing He, W. Zhao, Shuo Zhang, Haixia Du, Zhe-Fu Lin, Xiaojiang Han, Jingjun Peng
Abstract Cervical cancer is a typical cancer characterized by abnormal cell growth in the cervical area. Ginkgo biloba L. is a deciduous tree of the genus Ginkgo, possessing anti-cancer effects. The aim of this study was to explore the effect of strain J1 from Ginkgo biloba L. on apoptosis of cervical cancer cells. Bacteriostatic activity test, MTT assay and Flow cytometry were used in this study. Crude extract of J1 fermentation reduced cell growth in cervical cancer. The crude extract of the fermentation broth of strain J1 had a good inhibitory effect on Staphylococcus aureus. The crude extract of the J1 fermentation had no toxic effect on normal WISH cells in the range of anti-cervical cancer concentration. Crude extract of J1 fermentation induced apoptosis and regulated cell cycle in cervical cancer. The active compounds were separated and identified by preparative chromatography, and more than ten compounds were obtained. Our study suggests that the crude extract of J1 fermentation from Endophytic fungi of Ginkgo biloba reduced cell growth, and promoted apoptosis of cervical cancer, and is a potential therapeutic strategy for the treatment of cervical carcinoma.
{"title":"Crude extract of J1 fermentation promotes apoptosis of cervical cancer cells","authors":"Xia Yu, Qing He, W. Zhao, Shuo Zhang, Haixia Du, Zhe-Fu Lin, Xiaojiang Han, Jingjun Peng","doi":"10.1515/hc-2022-0161","DOIUrl":"https://doi.org/10.1515/hc-2022-0161","url":null,"abstract":"Abstract Cervical cancer is a typical cancer characterized by abnormal cell growth in the cervical area. Ginkgo biloba L. is a deciduous tree of the genus Ginkgo, possessing anti-cancer effects. The aim of this study was to explore the effect of strain J1 from Ginkgo biloba L. on apoptosis of cervical cancer cells. Bacteriostatic activity test, MTT assay and Flow cytometry were used in this study. Crude extract of J1 fermentation reduced cell growth in cervical cancer. The crude extract of the fermentation broth of strain J1 had a good inhibitory effect on Staphylococcus aureus. The crude extract of the J1 fermentation had no toxic effect on normal WISH cells in the range of anti-cervical cancer concentration. Crude extract of J1 fermentation induced apoptosis and regulated cell cycle in cervical cancer. The active compounds were separated and identified by preparative chromatography, and more than ten compounds were obtained. Our study suggests that the crude extract of J1 fermentation from Endophytic fungi of Ginkgo biloba reduced cell growth, and promoted apoptosis of cervical cancer, and is a potential therapeutic strategy for the treatment of cervical carcinoma.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":" ","pages":""},"PeriodicalIF":2.3,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48710607","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Abstract A series of novel quinazoline derivatives bearing sulfonamide moiety was designed and synthesized, and their structure were characterized by 1H NMR, 13C NMR, and HRMS techniques. Among them, the structure of compound E1 was further confirmed through X-ray single-crystal diffraction analyses. Their anti-Tobacco mosaic virus (TMV) activities were evaluated through half-leaf method. The bioassay results showed that E8 and E19 possess excellent inhibitory activity towards TMV. The EC50 of curative activities, protective activities, and inactivating activities of E8 and E19 are 132.1, 152.8, 57.4 mg/L and 278.0, 165.3, 94.5 mg/L, respectively, which are far superior than Ribavirin (318.2, 201.5, 128.6 mg/L, respectively).
{"title":"Design, synthesis, and antiviral activities evaluation of novel quinazoline derivatives containing sulfonamide moiety","authors":"Yixiang Deng, Shitao Yin, Xinyun Jing, Yu-Tao Zheng","doi":"10.1515/hc-2022-0160","DOIUrl":"https://doi.org/10.1515/hc-2022-0160","url":null,"abstract":"Abstract A series of novel quinazoline derivatives bearing sulfonamide moiety was designed and synthesized, and their structure were characterized by 1H NMR, 13C NMR, and HRMS techniques. Among them, the structure of compound E1 was further confirmed through X-ray single-crystal diffraction analyses. Their anti-Tobacco mosaic virus (TMV) activities were evaluated through half-leaf method. The bioassay results showed that E8 and E19 possess excellent inhibitory activity towards TMV. The EC50 of curative activities, protective activities, and inactivating activities of E8 and E19 are 132.1, 152.8, 57.4 mg/L and 278.0, 165.3, 94.5 mg/L, respectively, which are far superior than Ribavirin (318.2, 201.5, 128.6 mg/L, respectively).","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":" ","pages":""},"PeriodicalIF":2.3,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42300043","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Geoffrey P Wadey, Katrina E. Doherty, A. Sandoval, N. Leadbeater
Abstract Novel acyl pyrazoles and acyl triazoles have been prepared by means of the oxidative amidation of aldehydes in the presence of the requisite azole. Yields range from modest to good in both cases, and some limitations of the substrate scope have been discovered. Acyl pyrazoles were prepared by treatment of a mixture of aldehyde and pyrazole with an oxoammonium salt bearing the nitrate anion. In the case of acyl triazoles, the oxidative functionalization was performed using sodium persulfate as a terminal oxidant in the presence of a catalytic quantity of a nitroxide.
{"title":"Preparation of novel acyl pyrazoles and triazoles by means of oxidative functionalization reactions","authors":"Geoffrey P Wadey, Katrina E. Doherty, A. Sandoval, N. Leadbeater","doi":"10.1515/hc-2022-0158","DOIUrl":"https://doi.org/10.1515/hc-2022-0158","url":null,"abstract":"Abstract Novel acyl pyrazoles and acyl triazoles have been prepared by means of the oxidative amidation of aldehydes in the presence of the requisite azole. Yields range from modest to good in both cases, and some limitations of the substrate scope have been discovered. Acyl pyrazoles were prepared by treatment of a mixture of aldehyde and pyrazole with an oxoammonium salt bearing the nitrate anion. In the case of acyl triazoles, the oxidative functionalization was performed using sodium persulfate as a terminal oxidant in the presence of a catalytic quantity of a nitroxide.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":" ","pages":""},"PeriodicalIF":2.3,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46998743","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Maged F. El-Ahwany, Mohamed G. Assy, Mohamed H. Sherif, Mohamed R. Soliman, Abderrahim Titi, Rachid Touzani, Marwa S. El-Gendey, Wesam S. Shehab, Magda H. Abdellattif
Abstract In the drug chemistry industry, synthesizing a talented exclusive series of aza-polyheterocyclic compounds was crucial. Aminopyrimidine nucleus reacted with two equivalents of benzaldehyde in the presence of KOH as a starting material to bring about imidazopyrimidine derivative, which experienced intermolecular cyclization using carbon disulfide, Br 2 /AcOH, and/or HNO 2 to produce thiazole, thieno, and/or nitro pyrimidine derivative, respectively. Accordingly, the nucleus of Aminopyrimidine was prepared and used to develop the novel polyheterocyclic systems acylated with two moles of succinic anhydride to furnish the imidazolopyrimidine derivative. Benzylidene ethyl cyanoacetate and aminopyrimidine undergo (3 + 4) intermolecular cycloaddition 1,3 H shift followed by hydrolysis and after CO 2 evolution provided diazepine derivative. The diazepine derivative was attained due to the cyclo-condensation of the starting material and acetylacetone. Moreover, the structure of the novel synthesized compound series was exploited and verified via spectroscopic approaches. The synthesized series were tested for antimicrobial activity against gram-positive and gram-negative bacterial strains and antifungal activity. The thienopyrimidine derivatives and diazepine exhibited unusual antimicrobial activity. Furthermore, the molecular docking studies confirmed the biological studies with Molecular Operating Environment and petro orisis molinspiration studies, which proved the activity of compounds 4, 5, 7, 10, 13 , and 16 .
{"title":"Design, synthesis, biological evaluation, and bio-computational modeling of imidazo, thieno, pyrimidopyrimidine, pyrimidodiazepene, and motifs as antimicrobial agents","authors":"Maged F. El-Ahwany, Mohamed G. Assy, Mohamed H. Sherif, Mohamed R. Soliman, Abderrahim Titi, Rachid Touzani, Marwa S. El-Gendey, Wesam S. Shehab, Magda H. Abdellattif","doi":"10.1515/hc-2022-0156","DOIUrl":"https://doi.org/10.1515/hc-2022-0156","url":null,"abstract":"Abstract In the drug chemistry industry, synthesizing a talented exclusive series of aza-polyheterocyclic compounds was crucial. Aminopyrimidine nucleus reacted with two equivalents of benzaldehyde in the presence of KOH as a starting material to bring about imidazopyrimidine derivative, which experienced intermolecular cyclization using carbon disulfide, Br 2 /AcOH, and/or HNO 2 to produce thiazole, thieno, and/or nitro pyrimidine derivative, respectively. Accordingly, the nucleus of Aminopyrimidine was prepared and used to develop the novel polyheterocyclic systems acylated with two moles of succinic anhydride to furnish the imidazolopyrimidine derivative. Benzylidene ethyl cyanoacetate and aminopyrimidine undergo (3 + 4) intermolecular cycloaddition 1,3 H shift followed by hydrolysis and after CO 2 evolution provided diazepine derivative. The diazepine derivative was attained due to the cyclo-condensation of the starting material and acetylacetone. Moreover, the structure of the novel synthesized compound series was exploited and verified via spectroscopic approaches. The synthesized series were tested for antimicrobial activity against gram-positive and gram-negative bacterial strains and antifungal activity. The thienopyrimidine derivatives and diazepine exhibited unusual antimicrobial activity. Furthermore, the molecular docking studies confirmed the biological studies with Molecular Operating Environment and petro orisis molinspiration studies, which proved the activity of compounds 4, 5, 7, 10, 13 , and 16 .","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"21 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135102658","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Abstract Due to the chemical properties of Group VIII transition metals and their importance in catalytic processes, the reactions of rhodium and its neighboring organic complexes have received much attention as model systems. In the present experiments, we successfully prepared two new rhodium complexes named [Rh(cod)(TTP)Cl] and [Rh(cod)(CDP)Cl] using tri( o -tolyl)phosphine and clohexyldiphenylphosphine as ligands, respectively, and the proofs of their structures were completed using 1 H NMR and 13 C NMR. Subsequently, it was applied to the polymerization reaction of phenylacetylene (PA), and the effects of different solvents, time, and temperature on the yield and molecular weight of the polymerization reaction products were discussed. The experimental results show that both complexes can play a catalytic role in the polymerization of PA. From the point of view of polymer molecular weight, the best reaction conditions for both catalysts were 3 h at 20°C in THF solvent (molecular weight up to 2.40 × 10 5 ). From the point of view of yield, the best reaction conditions for both catalysts were 4 h at 35°C in THF solvent (yield up to 89.2%).
{"title":"Synthesis of a novel phosphate-containing ligand rhodium catalyst and exploration of its optimal reaction conditions and mechanism for the polymerization of phenylacetylene","authors":"Mingyu Zhang, Yuqi Tang, Rui Xu, Dong Yan, Shuangping Xu, Yanqing Qu, Jingyu Xu, Hongge Jia","doi":"10.1515/hc-2022-0163","DOIUrl":"https://doi.org/10.1515/hc-2022-0163","url":null,"abstract":"Abstract Due to the chemical properties of Group VIII transition metals and their importance in catalytic processes, the reactions of rhodium and its neighboring organic complexes have received much attention as model systems. In the present experiments, we successfully prepared two new rhodium complexes named [Rh(cod)(TTP)Cl] and [Rh(cod)(CDP)Cl] using tri( o -tolyl)phosphine and clohexyldiphenylphosphine as ligands, respectively, and the proofs of their structures were completed using 1 H NMR and 13 C NMR. Subsequently, it was applied to the polymerization reaction of phenylacetylene (PA), and the effects of different solvents, time, and temperature on the yield and molecular weight of the polymerization reaction products were discussed. The experimental results show that both complexes can play a catalytic role in the polymerization of PA. From the point of view of polymer molecular weight, the best reaction conditions for both catalysts were 3 h at 20°C in THF solvent (molecular weight up to 2.40 × 10 5 ). From the point of view of yield, the best reaction conditions for both catalysts were 4 h at 35°C in THF solvent (yield up to 89.2%).","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"28 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135498094","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Abstract A series of novel 4,6-dimorpholinyl-1,3,5-triazine derivatives 6a–6r were obtained through N-substitution and Claisen-Schmidt condensation. 1H NMR, 13C NMR, and mass spectrometry were used to characterize the molecular structures of the derivatives. The in vitro antiproliferation activity of derivatives was evaluated using the MTT assay against SW620 (human colon cancer cells), A549 (human nonsmall cell lung cancer cells), HeLa (human cervical cancer cells), and MCF-7 (human breast cancer cells). Compound 6o bearing a pyridyl group exhibited good cytotoxicity against four cancer cells, with IC50 values of 8.71, 9.55, 15.67, and 21.77 μM, sequentially. In addition, compound 6a showed some selectivity against SW620. Graphical abstract The chalcone structure was introduced into the 4,6-dimorpholinyl-1,3,5-triazine molecule through the C-N bond, and a series of new compounds were obtained. Among them, the pyridyl-containing 6o exhibits anti-proliferation activity similar to that of cisplatin on SW620. Interestingly, the phenyl-containing 6a exhibits a certain selectivity for the anti-proliferation activity of SW620.
{"title":"Design, synthesis, and anticancer activity of novel 4,6-dimorpholinyl-1,3,5-triazine compounds","authors":"Jinjing Li, Linbo Li, Yuxiao Liu, Jie Zhang, Cheng Shi, Shujing Zhou, Hongbin Qiu","doi":"10.1515/hc-2022-0152","DOIUrl":"https://doi.org/10.1515/hc-2022-0152","url":null,"abstract":"Abstract A series of novel 4,6-dimorpholinyl-1,3,5-triazine derivatives 6a–6r were obtained through N-substitution and Claisen-Schmidt condensation. 1H NMR, 13C NMR, and mass spectrometry were used to characterize the molecular structures of the derivatives. The in vitro antiproliferation activity of derivatives was evaluated using the MTT assay against SW620 (human colon cancer cells), A549 (human nonsmall cell lung cancer cells), HeLa (human cervical cancer cells), and MCF-7 (human breast cancer cells). Compound 6o bearing a pyridyl group exhibited good cytotoxicity against four cancer cells, with IC50 values of 8.71, 9.55, 15.67, and 21.77 μM, sequentially. In addition, compound 6a showed some selectivity against SW620. Graphical abstract The chalcone structure was introduced into the 4,6-dimorpholinyl-1,3,5-triazine molecule through the C-N bond, and a series of new compounds were obtained. Among them, the pyridyl-containing 6o exhibits anti-proliferation activity similar to that of cisplatin on SW620. Interestingly, the phenyl-containing 6a exhibits a certain selectivity for the anti-proliferation activity of SW620.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":" ","pages":""},"PeriodicalIF":2.3,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49372391","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Abstract Lung cancer shows a high rate of incidence and mortality. This study aimed to investigate the influence of octreotide (OCT) on lipopolysaccharide (LPS)-induced apoptosis and metabolome expression in A549 cells. After A549 cells were treated by LPS or co-cultured with LPS and OCT, cell apoptosis was tested by flow cytometry, and gas chromatography-mass spectrometer (GC/MS) and high-performance liquid chromatography-mass spectrometer (LC/MS) were subjected to determine the differently expressed metabolites, and the interaction network was constructed. Results found that OCT promoted the apoptosis of A549 cells and significantly affected LPS-regulated cell apoptosis. Following the further investigation by orthogonal partial least squares discriminant analysis (OPLS-DA), the metabolites with different expression levels were obtained, and most of which belong to amino acids, phospholipids, organic acid, and saccharides. Fourteen components with the role of the marker metabolites included serotonin, indole, threonine, serine, glucose, phenylalanine, lactose, fumarate, 4-hydroxyphenyllactate, aspartate, asparagine, putrescine, proline, and succinate. It is indicated that OCT promotes apoptosis through five metabolism pathways and 14 key metabolism elements in A549 cells.
{"title":"Influence of octreotide on apoptosis and metabolome expression in lipopolysaccharide-induced A549 cells","authors":"Luoyang Ruan, Xiaomeng Xu, Jinliang Cao, Xiaohong Xu","doi":"10.1515/hc-2022-0159","DOIUrl":"https://doi.org/10.1515/hc-2022-0159","url":null,"abstract":"Abstract Lung cancer shows a high rate of incidence and mortality. This study aimed to investigate the influence of octreotide (OCT) on lipopolysaccharide (LPS)-induced apoptosis and metabolome expression in A549 cells. After A549 cells were treated by LPS or co-cultured with LPS and OCT, cell apoptosis was tested by flow cytometry, and gas chromatography-mass spectrometer (GC/MS) and high-performance liquid chromatography-mass spectrometer (LC/MS) were subjected to determine the differently expressed metabolites, and the interaction network was constructed. Results found that OCT promoted the apoptosis of A549 cells and significantly affected LPS-regulated cell apoptosis. Following the further investigation by orthogonal partial least squares discriminant analysis (OPLS-DA), the metabolites with different expression levels were obtained, and most of which belong to amino acids, phospholipids, organic acid, and saccharides. Fourteen components with the role of the marker metabolites included serotonin, indole, threonine, serine, glucose, phenylalanine, lactose, fumarate, 4-hydroxyphenyllactate, aspartate, asparagine, putrescine, proline, and succinate. It is indicated that OCT promotes apoptosis through five metabolism pathways and 14 key metabolism elements in A549 cells.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":" ","pages":""},"PeriodicalIF":2.3,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42898801","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Abstract A series of novel 1,2,4-triazole-chalcone compounds 10a–10s were designed by molecular hybridization strategy and synthesized. The molecular structures of the novel chalcones were characterized by 1 H-NMR, 13 C-NMR, and HRMS. The anti-proliferative activities of the novel chalcones against four cancer cell lines in vitro were examined by MTT, four tumor cell lines including human colon cancer cell SW620, human non-small cell lung cancer cell A549, human cervical cancer cell HeLa, and human breast cancer cell MCF-7. Compound 10o showed certain selectivity to SW620 cell line, and its IC 50 value was 21.55 μM. 10q had good anti-proliferative activity against A549 cells with an IC 50 value of 25.58 μM.
{"title":"Design, synthesis, and antiproliferative activity of novel 1,2,4-triazole-chalcone compounds","authors":"Jinjing Li, Pingping Fan, Yuxiao Liu, Yan Zhao, Chengyang Shi, Shujing Zhou, Hongbin Qiu","doi":"10.1515/hc-2022-0165","DOIUrl":"https://doi.org/10.1515/hc-2022-0165","url":null,"abstract":"Abstract A series of novel 1,2,4-triazole-chalcone compounds 10a–10s were designed by molecular hybridization strategy and synthesized. The molecular structures of the novel chalcones were characterized by 1 H-NMR, 13 C-NMR, and HRMS. The anti-proliferative activities of the novel chalcones against four cancer cell lines in vitro were examined by MTT, four tumor cell lines including human colon cancer cell SW620, human non-small cell lung cancer cell A549, human cervical cancer cell HeLa, and human breast cancer cell MCF-7. Compound 10o showed certain selectivity to SW620 cell line, and its IC 50 value was 21.55 μM. 10q had good anti-proliferative activity against A549 cells with an IC 50 value of 25.58 μM.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"4 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135211049","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Zhili Fang, Hui Zhang, Ping Wang, Xiaoguang Li, Qixiang Nie
Abstract In this study, metal–organic nanofibers (MONFs) and reduced graphite oxide (rGO) nanocomposite were used to modify the surface of glassy carbon electrode, and the electrochemical sensor was applied to the differential pulse voltammetry determination of hypoxanthine, the oxidation intermediate of human purine degradation metabolism. The preparation of MONFs/rGO nanocomposite is simple, efficient, and environmentally friendly. The morphology and structure of MONFs/rGO nanocomposite were characterized by field emission scanning electron microscopy and X-ray diffraction. The results show that the improved sensor has a significant increase in current density, with linear ranges of 0.1–10 and 20–100 μM. Detection limit 0.01 μM ( S / N = 3). Under the optimized conditions, the improved sensor shows very good stability, selectivity, and improved accuracy.
摘要本研究采用金属有机纳米纤维(MONFs)和还原氧化石墨(rGO)纳米复合材料修饰玻碳电极表面，并将电化学传感器应用于差分脉冲伏安法测定人体嘌呤降解代谢氧化中间体次黄嘌呤。MONFs/rGO纳米复合材料的制备简单、高效、环保。采用场发射扫描电镜和x射线衍射对MONFs/rGO纳米复合材料的形貌和结构进行了表征。结果表明，改进后的传感器电流密度显著提高，线性范围为0.1 ~ 10 μM和20 ~ 100 μM。检测限为0.01 μM (S / N = 3)。在优化条件下，改进后的传感器具有良好的稳定性、选择性和精度。
{"title":"Synthesis of metal–organic nanofiber/rGO nanocomposite as the sensing element for electrochemical determination of hypoxanthine","authors":"Zhili Fang, Hui Zhang, Ping Wang, Xiaoguang Li, Qixiang Nie","doi":"10.1515/hc-2022-0166","DOIUrl":"https://doi.org/10.1515/hc-2022-0166","url":null,"abstract":"Abstract In this study, metal–organic nanofibers (MONFs) and reduced graphite oxide (rGO) nanocomposite were used to modify the surface of glassy carbon electrode, and the electrochemical sensor was applied to the differential pulse voltammetry determination of hypoxanthine, the oxidation intermediate of human purine degradation metabolism. The preparation of MONFs/rGO nanocomposite is simple, efficient, and environmentally friendly. The morphology and structure of MONFs/rGO nanocomposite were characterized by field emission scanning electron microscopy and X-ray diffraction. The results show that the improved sensor has a significant increase in current density, with linear ranges of 0.1–10 and 20–100 μM. Detection limit 0.01 μM ( S / N = 3). Under the optimized conditions, the improved sensor shows very good stability, selectivity, and improved accuracy.","PeriodicalId":12914,"journal":{"name":"Heterocyclic Communications","volume":"55 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135560271","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：