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کاربرد نوع شرط:
- جایگاه : پژوهشی
- مجله: Journal of Medicinal and Chemical Sciences
- نوع مقاله: Journal Article
- کلمات کلیدی: Antibacterial,Antioxidant property,Pyrazoles,Heterocyclic compounds,3-methyl-5-pyrazolone derivatives,Pyrazolone,protein kinase inhibition
- چکیده:
- چکیده انگلیسی: Recently, infectious diseases have increased enormously, causing a major threat to public health despite the marvelous progress in the medicinal chemistry. Fused pyrazole derivatives are having a wide range of pharmacological activities, playing a vital role as potential therapeutic agents in various pathological conditions. In the present study, novel fused pyrazoles derivatives were synthesized and evaluated for protein kinase inhibition, antioxidant, and antimicrobial activities. 3-Methyl-5-pyrazolone was first prepared by treating ethyl acetoacetate with hydrazine hydrate in absolute ethanol. Then it was treated with different aromatic aldehydes (benzaldehyde, salicylaldehyde, vanillin, 4-diamethylaminobanzaldehyde, and cinnamaldehyde) to form benzylidene derivatives of pyrazoles. These substituted pyrazoles were then treated with hydrazine and phenylhydrazine to produce fused pyrazole ring systems. The synthesized compounds were purified by recrystallization, and then characterized using the spectroscopic techniques. All the compounds exhibited moderate antibacterial activity. Antioxidant potential was determined by three methods and most of the compounds exhibited good antioxidant potential. Two compounds including, 5a and 5e demonstrated protein kinase inhibitory activity. The results indicated that, the fused pyrazoles ring systems possess prominent biological properties.
- انتشار مقاله: 13-06-1399
- نویسندگان: Fazli Azim,Humaira Nadeem,Muhammad Imran,Shagufta Naz,Ihsan-ul- Haq,Nawshad Muhammad,Aneela Hayat,Md Shahidul Islam
- مشاهده
- جایگاه : پژوهشی
- مجله: Asian Pacific Journal of Cancer Prevention
- نوع مقاله: Journal Article
- کلمات کلیدی: Apoptosis,miRNAs,Glioblastoma,miR-4731
- چکیده:
- چکیده انگلیسی: GBM (Glioblastoma multiforme) is the most prevalent and lethal primary brain tumor. Gene therapy is one of the promising approaches and involves the delivery of genetic therapeutic molecules for specific antitumour response/activity. miRNAs can regulate the cell biology functions including replication, cell growth, and apoptosis by regulating gene expression. In this study, we found that down-regulation of miR-4731 expression occurred in GBM cells. We further determined that miR-4731 behaved as a tumor suppressor by inhibiting GBM cell proliferation. We further investigated the molecular mechanisms of miR-4731 and EGFR, ERK-1,2 and AKT-1,2 in GBM cell lines U87 and U251. The in vitro ectopic expression of miR-4731 affected cell proliferation, migration, and invasion of U87 and U251 cells. Luciferase reporter assays validated that miR-4731 targeted the 3′-untranslated region (3′-UTR) of EGFR. In conclusions, we identified that miR-4731 plays a tumor suppressor role in GBM cell proliferation and migration by targeting EGFR expression, and miR-4731 may act as a novel biomarker for early diagnosis or therapeutic target of GBM.
- انتشار مقاله: 05-10-1398
- نویسندگان: Amir Alahverdi,Ehsan Arefian,Masoud Soleimani,Jafar Ai,Aaliakbar Yousefi-Ahmadipour,Abouzar Babaei,Md Shahidul Islam,Somayeh Ebrahimi-Barough
- مشاهده