Design and In Vitro Evaluation of Schiff Base-Based Heterocyclic Derivatives as Potential Anticancer Agents Targeting Pancreatic Cancer.
Background & Objective: Pancreatic cancer is a highly aggressive malignancy that necessitates the development of novel chemotherapeutic agents with improved selectivity and efficacy. This study aimed to synthesize and biologically evaluate a series of Schiff base derivatives as potential anticancer...
| Publicado en: | Journal of Advances in Medical & Biomedical Research Vol. 34; no. 2; pp. 193 - 200 |
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| Autores principales: | , , |
| Formato: | pictorial research tables/charts Journal Article |
| Publicado: |
Zanjan University of Medical Sciences & Health Services
Mar/Apr2026
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| Acceso en línea: | Ver este registro en EBSCOhost |
| fields | @attributes: recordID: 1 pdfLink: plink: https://search.ebscohost.com/login.aspx?direct=true&db=ccm&AN=195814696&site=ehost-live header: @attributes: shortDbName: ccm uiTerm: 195814696 longDbName: CINAHL Complete uiTag: AN controlInfo: bkinfo: dissinfo: jinfo: jid: 26766264 N5MJ jtl: Journal of Advances in Medical & Biomedical Research issn: 26766264 maglogo: N pubinfo: dt: Mar/Apr2026 vid: 34 iid: 2 pid: 65276 pub: Zanjan University of Medical Sciences & Health Services artinfo: ui: 195814696 195814696 195814696 10.30699/jambr.34.2.193 195814696 ppf: 193 ppct: 7 formats: fmt: @attributes: type: P tig: atl: Design and In Vitro Evaluation of Schiff Base-Based Heterocyclic Derivatives as Potential Anticancer Agents Targeting Pancreatic Cancer. aug: au: Ali, Dina Naseer Ahmed, Ahmed Al-qaisi, Alaa Hussein J. affil: Department of Microbial Biotechnology, College of Biotechnology, AL-Nahrain University, Jadriga, Baghdad, Iraq. sug: subj: Organic Chemicals Therapeutic Use Heterocyclic Compounds Therapeutic Use Heterocyclic Compounds Analogs and Derivatives Antineoplastic Agents Therapeutic Use Pancreatic Neoplasms Drug Therapy Apoptosis Drug Effects Treatment Outcomes Human Iraq Molecular Structure In Vitro Studies Experimental Studies Caspases Cell Cycle Indicators and Reagents One-Way Analysis of Variance Post Hoc Analysis Data Analysis Software Azepines Sulfur Compounds Cell Proliferation ab: Background & Objective: Pancreatic cancer is a highly aggressive malignancy that necessitates the development of novel chemotherapeutic agents with improved selectivity and efficacy. This study aimed to synthesize and biologically evaluate a series of Schiff base derivatives as potential anticancer agents against pancreatic cancer by assessing their cytotoxicity, selectivity, and ability to induce apoptosis in vitro. Materials & Methods: A different novel heterocyclic derivative, including dihydroquinazoline, oxazepine, tetrazole, and thiazine, were synthesized via a common Schiff base intermediate (Derivative D). The structural characterization of these compounds was performed using FTIR and 1^11H-NMR spectroscopy. To evaluate their therapeutic potential and selectivity, the synthesized derivatives were tested in vitro against PANC-1 (pancreatic cancer) and HDFn (normal human dermal fibroblast) cell lines. Results: MTT assays demonstrated dose-dependent inhibition of cell proliferation by all synthesized compounds. Among them, derivative D4 exhibited greater selectivity toward pancreatic cancer cells, with IC₅₀ values of 129.5 μg/mL for PANC-1 cells and 237.4 μg/mL for HDFn cells. In contrast, derivative D5 showed greater overall cytotoxicity but lower selectivity, with IC₅₀ values of 68.9 μg/mL for PANC-1 cells and 61.0 μg/mL for HDFn cells. High-content screening revealed that D4 treatment significantly reduced the number of viable cells and decreased mitochondrial membrane potential, accompanied by increased nuclear intensity and cell membrane permeability. Furthermore, D4 significantly activated both caspase-8 and caspase-9 at concentrations of 100 and 200 μg/mL (P = 0.0019 and P < 0.0001, respectively), indicating activation of both the extrinsic and intrinsic apoptotic pathways. Conclusion: These findings suggest that the structural optimization of Schiff base-derived heterocycles is a promising strategy for enhancing tumor selectivity and biological safety, potentially offering new avenues for anticancer therapy. pubtype: Academic Journal doctype: pictorial research tables/charts Journal Article ougenre: Article language: English refInfo: holdings: @attributes: islocal: N |
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