Background: A series of benzimidazole derivatives was developed and its chemical scaffolds were authenticated by NMR, IR, elemental analyses and physicochemical properties. The synthesized compounds were screened for their antimicrobial and antiproliferative activities.
Results And Discussion: The synthesized benzimidazole compounds were evaluated for their antimicrobial activity using the tube dilution method and were found to exhibit good antimicrobial potential against selected Gram negative and positive bacterial and fungal species. The compounds were also assessed for their anticancer activity exhibited using the SRB assay and were found to elicit antiproliferative activity against MCF7 breast cancer cell line, which was comparable to the standard drug.
Conclusion: Antimicrobial screening results indicated that compounds 1, 2 and 19 to be promising antimicrobial agents against selected microbial species and comparable to standard drugs which included norfloxacin and fluconazole. The anticancer screening results revealed that compounds, 12, 21, 22 and 29 to show the highest activity against MCF7 and their IC values were more potent than 5-fluorouracil.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6768139 | PMC |
| http://dx.doi.org/10.1186/s13065-018-0498-y | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Novel Dehydroabietylamine C-Ring Schiff Base Derivatives: Synthesis, Antiproliferative activity, DNA binding and Molecular docking.
Chem Asian J
January 2025
Nanjing Forestry University, College of Science, CHINA.
A series of Dehydroabietylamine (DHAA) C-ring Schiff derivatives, L3-L20, were synthesized and their in vitro cytotoxic activity against the human tumor cell lines cervix HeLa, breast MCF-7, lung A549, liver HepG2, and the nonmalignant cell line umbilical vein HUVEC was investigated. Most of the compounds showed varying degrees of anticancer activity against HeLa cell lines while demonstrating lower toxicity to normal HUVEC cells compared to DHAA and doxorubicin (DOX), especially compound L19, which not only enhanced the anticancer activity of DHAA, but also significantly reduced the toxicity to normal cells, achieving a selectivity index (SI) 118 times higher than that of DHAA and 245 times higher than that of DOX. In addition, compound L19 induced apoptosis in HeLa cells in a dose-dependent manner and arrested the cell cycle in S phase.
View Article and Find Full Text PDFThree new diterpenes from the roots of Salvia miltiorrhiza and their cytotoxicity.
Fitoterapia
January 2025
School of Biological Sciences and Technology, University of Jinan, Jinan 250022, China; Shandong Engineering Research Center of Key Technologies for High-Value and High-Efficiency Full Industry Chain of Lonicera japonica, Linyi 273399, China. Electronic address:
Two undescribed oxazole-containing diterpenoids (1-2) and a new diterpenoid (3) were isolated from the roots of Salvia miltiorrhiza. Their structures were elucidated by extensive HRESIMS and NMR spectroscopic analysis, and the absolute configurations of 1 and 3 were confirmed by comparison of the calculated and experimental electronic circular dichroism (ECD) spectra. Compound 1 represents the first example of an abietane diterpenoid with a benzo[d]oxazole unit fused in the ring B of the abietane skeleton.
View Article and Find Full Text PDFTherapeutic potential of brentuximab vedotin in breast cancer and lymphoma via targeted apoptosis and gene regulation.
Sci Rep
January 2025
Department of Medical Biotechnology, College of Biotechnology, Misr University for Science and Technology, P. O. Box 77, Giza, Egypt.
This study was designed to assess the effect of brentuximab vedotin on several breast cancer cell lines in terms of promoting apoptosis and managing cancer progression. Additionally, the study investigated the potential of repurposing this drug for new therapeutic reasons, beyond its original indications. The study evaluates the cytotoxic effects of Brentuximab vedotin across five cell lines: normal human skin fibroblasts (HSF), three breast cancer cell lines (MCF-7, MDA-MB-231, and T-47D), and histiocytic lymphoma (U-937).
View Article and Find Full Text PDFEvaluation of the interaction between Menthol and Camphor, Major Compounds of Clinopodium nepeta Essential Oil: Antioxidant, Anti-inflammatory and Anticancer Activities against Breast Cancer Cell Lines.
Chem Biodivers
January 2025
Mohammed I University Oujda: Universite Mohammed Premier Oujda, Biology department, BV Mohammed VI B.P. 524 Oujda, Oujda, 60000, Oujda, MOROCCO.
This study evaluates the antioxidant, anti-inflammatory and anticancer activities of camphor, menthol and their equimolar combination. In silico toxicity analysis confirmed the absence of toxic effects for both compounds. Antioxidant activity, assessed by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays, revealed a synergistic effect of the equimolar combination with IC50 values of 10.
View Article and Find Full Text PDFThe eukaryotic genome is packaged into chromatin, which is composed of a nucleosomal filament that coils up to form more compact structures. Chromatin exists in two main forms: euchromatin, which is relatively decondensed and enriched in transcriptionally active genes, and heterochromatin, which is condensed and transcriptionally repressed . It is widely accepted that chromatin architecture modulates DNA accessibility, restricting the access of sequence-specific, gene-regulatory, transcription factors to the genome.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!