A new synthesized benzene nitrogen mustard was converted into glycosyl donor-trichloroacetimidate that was glycosylated with p-nitrophenol（glycosyl donors） to form β-lactosyl p-nitrobenzene under the protection of ...A new synthesized benzene nitrogen mustard was converted into glycosyl donor-trichloroacetimidate that was glycosylated with p-nitrophenol（glycosyl donors） to form β-lactosyl p-nitrobenzene under the protection of acetyl in a stereoselective manner, was prepared and evaluated for its cytotoxicity towards cultured K562 cell line. Methylthiazoy tetrazolium（MTT） assay, transmission electron microscopy（TEM）, flow cytometry（FCM） and immunohistochemistry were utilized to explore the mechanisms of how the compound arrests the growth of HCT-T cells. This new synthesed benzene nitrogen mustard glucoside derivate（BNMGD） presented a lower toxicity to normal cells, but is significantly more toxic to K562 cells compared with nitrogen mustard, meanwhile it can induce the apoptosis of K562 cells. These results indicate that the new synthesized BNMGD can inhibit the growth of K562 cells and induce the apoptosis, and its cytotoxicity towards cultured K562 cell line is much more effective than that of nitrogen mustard.展开更多
Antibody-directed enzyme prodrug therapy（ADEPT） is a new strategy for the treatment of cancer that has arisen in recent twenty years, the main merits of which are that it can improve the selectivity of anticancer dr...Antibody-directed enzyme prodrug therapy（ADEPT） is a new strategy for the treatment of cancer that has arisen in recent twenty years, the main merits of which are that it can improve the selectivity of anticancer drugs and reduce the side effects in remote tissue. In the present study, two prodrugs-glycosylated aromatic nitrogen mustard derivatives were synthesized. Glucose and lactose were converted into glycosyl donors-trichloroacetimidate; the obtained glycosyl donors were glycosylated with p-nitrophenol （ glycosyl donors） to form β-glucosyl p-nitrobenzene and β-lactosyl p-nitrobenzene that were protected by acetyl in a stereoselective manner; the two products were reduced by zinc dust and then treated with ethylene oxide, afforded two glycosylated nitrogen mustard derivatives that were protected by acetyl; the last step was to deacetylate and then afforded the two target compounds that could be used as prodrugs of ADEPT for further Anti-tumor research.展开更多
Two novel steroid-linked nitrogen mustard conjugates la and lb were synthesized by using estrogenic acid 4 coupled with aniline mustard 8 and phenol mustard 13 in an esterification or amidation procedure. Preliminary ...Two novel steroid-linked nitrogen mustard conjugates la and lb were synthesized by using estrogenic acid 4 coupled with aniline mustard 8 and phenol mustard 13 in an esterification or amidation procedure. Preliminary cytotoxic screening on cancer cell lines in vitro showed that, the steroid-ester linked nitrogen mustard conjugate la exhibited obvious increasing of activities.展开更多
The study, conducted at the Research Farm of the College of Agriculture, University of Tabriz in 2021, focused on the effects of various nitrogen-fixing bacterial isolates, biofertilizers containing nitrogen and phosp...The study, conducted at the Research Farm of the College of Agriculture, University of Tabriz in 2021, focused on the effects of various nitrogen-fixing bacterial isolates, biofertilizers containing nitrogen and phosphorus, as well as iron and zinc foliar applications on mustard growth under rainfed conditions. The results indicated that biofertilizers, whether used alone or in combination with chemical fertilizers, produced comparable grain and oil outputs compared to chemical fertilizers alone. Additionally, the application of iron and zinc through foliar spraying significantly enhanced both grain and oil production. These findings suggest that integrating nitrogen-fixing bacteria and biofertilizers could reduce reliance on chemical nitrogenous fertilizers, leading to decreased production expenses, improved product quality, and minimized environmental impact. This study highlights the potential for sustainable agricultural practices in dry land farming as a viable alternative to traditional chemical-intensive methods. Substituting chemical nitrogenous fertilizers with nitrogen-fixing bacteria or biofertilizers could result in cost savings in mustard grain and oil production while promoting environmental sustainability.展开更多
The thiophene-derived amido bis-nitrogen mustard N2,N2,N5,N5-tetrakis（2-chloroethyl）-3,4-dimethylthio- phene-2,5-dicarboxamide was designed and synthesized via five-step reactions from commercially available 2-chlor...The thiophene-derived amido bis-nitrogen mustard N2,N2,N5,N5-tetrakis（2-chloroethyl）-3,4-dimethylthio- phene-2,5-dicarboxamide was designed and synthesized via five-step reactions from commercially available 2-chloroacetonitrile. This target compound was confirmed by 1H NMR, 13C NMR, MS, IR spectra and elemental analyses, and its structure was further characterized by X-ray single-crystal analysis. The biological activities for the title compound and some intermediates were evaluated in vitro for their antibacterial, antifungal and cytotoxic activities. The preliminary results showed that the title compound could inhibit efficiently the growth of the tested microorganisms including drug-resistant bacteria MRSA to some extent. Moreover, the target compound was found to be effective against prostatic carcinoma cell line （PC-3）, breast carcinoma cell line （MCF-7）, colon carcinoma （LoVo） and lung cancer （A549）. Especially, it gave selective antitumor efficacy against prostatic carcinoma cell line （PC-3） at a low dose. Keywords nitrogen mustard, thiophene, antibacterial, antifungal, cytotoxicity展开更多
2,7,12,18-Tetramethyl-13,17-di[3'-N,N'-di(2'-chloroethyl)aminopropyl]porphin and it's 3,8-di(1'-alkyloxyethyl)-analogous or porphyrin-nitrogen mustards were synthesized for the first time Their str...2,7,12,18-Tetramethyl-13,17-di[3'-N,N'-di(2'-chloroethyl)aminopropyl]porphin and it's 3,8-di(1'-alkyloxyethyl)-analogous or porphyrin-nitrogen mustards were synthesized for the first time Their structures were determined by spectroscopics and elemental analyses.Most of the compounds possess both the chemotherapeutic and photodynamic effects on tumor and deserve further investigation.展开更多
基金Supported by the Department of Jilin Province Technology, China(No.20070417)
文摘A new synthesized benzene nitrogen mustard was converted into glycosyl donor-trichloroacetimidate that was glycosylated with p-nitrophenol（glycosyl donors） to form β-lactosyl p-nitrobenzene under the protection of acetyl in a stereoselective manner, was prepared and evaluated for its cytotoxicity towards cultured K562 cell line. Methylthiazoy tetrazolium（MTT） assay, transmission electron microscopy（TEM）, flow cytometry（FCM） and immunohistochemistry were utilized to explore the mechanisms of how the compound arrests the growth of HCT-T cells. This new synthesed benzene nitrogen mustard glucoside derivate（BNMGD） presented a lower toxicity to normal cells, but is significantly more toxic to K562 cells compared with nitrogen mustard, meanwhile it can induce the apoptosis of K562 cells. These results indicate that the new synthesized BNMGD can inhibit the growth of K562 cells and induce the apoptosis, and its cytotoxicity towards cultured K562 cell line is much more effective than that of nitrogen mustard.
基金Supported by the National Natural Science Foundation of China(No20030708)the Natural Science Foundation of JinlinProrince, P R China(No20050702-4)
文摘Antibody-directed enzyme prodrug therapy（ADEPT） is a new strategy for the treatment of cancer that has arisen in recent twenty years, the main merits of which are that it can improve the selectivity of anticancer drugs and reduce the side effects in remote tissue. In the present study, two prodrugs-glycosylated aromatic nitrogen mustard derivatives were synthesized. Glucose and lactose were converted into glycosyl donors-trichloroacetimidate; the obtained glycosyl donors were glycosylated with p-nitrophenol （ glycosyl donors） to form β-glucosyl p-nitrobenzene and β-lactosyl p-nitrobenzene that were protected by acetyl in a stereoselective manner; the two products were reduced by zinc dust and then treated with ethylene oxide, afforded two glycosylated nitrogen mustard derivatives that were protected by acetyl; the last step was to deacetylate and then afforded the two target compounds that could be used as prodrugs of ADEPT for further Anti-tumor research.
基金support of the National Natural Science Foundation of China(No.20672050)
文摘Two novel steroid-linked nitrogen mustard conjugates la and lb were synthesized by using estrogenic acid 4 coupled with aniline mustard 8 and phenol mustard 13 in an esterification or amidation procedure. Preliminary cytotoxic screening on cancer cell lines in vitro showed that, the steroid-ester linked nitrogen mustard conjugate la exhibited obvious increasing of activities.
文摘The study, conducted at the Research Farm of the College of Agriculture, University of Tabriz in 2021, focused on the effects of various nitrogen-fixing bacterial isolates, biofertilizers containing nitrogen and phosphorus, as well as iron and zinc foliar applications on mustard growth under rainfed conditions. The results indicated that biofertilizers, whether used alone or in combination with chemical fertilizers, produced comparable grain and oil outputs compared to chemical fertilizers alone. Additionally, the application of iron and zinc through foliar spraying significantly enhanced both grain and oil production. These findings suggest that integrating nitrogen-fixing bacteria and biofertilizers could reduce reliance on chemical nitrogenous fertilizers, leading to decreased production expenses, improved product quality, and minimized environmental impact. This study highlights the potential for sustainable agricultural practices in dry land farming as a viable alternative to traditional chemical-intensive methods. Substituting chemical nitrogenous fertilizers with nitrogen-fixing bacteria or biofertilizers could result in cost savings in mustard grain and oil production while promoting environmental sustainability.
文摘The thiophene-derived amido bis-nitrogen mustard N2,N2,N5,N5-tetrakis（2-chloroethyl）-3,4-dimethylthio- phene-2,5-dicarboxamide was designed and synthesized via five-step reactions from commercially available 2-chloroacetonitrile. This target compound was confirmed by 1H NMR, 13C NMR, MS, IR spectra and elemental analyses, and its structure was further characterized by X-ray single-crystal analysis. The biological activities for the title compound and some intermediates were evaluated in vitro for their antibacterial, antifungal and cytotoxic activities. The preliminary results showed that the title compound could inhibit efficiently the growth of the tested microorganisms including drug-resistant bacteria MRSA to some extent. Moreover, the target compound was found to be effective against prostatic carcinoma cell line （PC-3）, breast carcinoma cell line （MCF-7）, colon carcinoma （LoVo） and lung cancer （A549）. Especially, it gave selective antitumor efficacy against prostatic carcinoma cell line （PC-3） at a low dose. Keywords nitrogen mustard, thiophene, antibacterial, antifungal, cytotoxicity
文摘2,7,12,18-Tetramethyl-13,17-di[3'-N,N'-di(2'-chloroethyl)aminopropyl]porphin and it's 3,8-di(1'-alkyloxyethyl)-analogous or porphyrin-nitrogen mustards were synthesized for the first time Their structures were determined by spectroscopics and elemental analyses.Most of the compounds possess both the chemotherapeutic and photodynamic effects on tumor and deserve further investigation.
