吡唑类化合物抗多形性胶质母细胞瘤的抗癌活性研究:合成、体外及分子对接研究

IF 1.9 4区 医学 Q3 CHEMISTRY, MEDICINAL Medicinal Chemistry Pub Date : 2025-01-17 DOI:10.2174/0115734064337582241103172720
Kemal Alp Nalcı, Cihat Mete, Zeynep Demir, İshak Bildirici, Adnan Cetin
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引用次数: 0

摘要

背景:多形式胶质母细胞瘤(GBM)是一种高度侵袭性和流行的脑癌,男性发病率较高,由于耐药、癌细胞靶向和渗透不足以及对其分子途径的不完全了解,治疗成功率有限。GBM是一种高度侵袭性的脑癌,治疗选择有限。本研究探讨了合成的吡唑类化合物对GBM细胞的抗癌潜力。方法:合成一系列吡唑衍生物,采用MTT法测定其抗GBM的疗效。通过分子对接研究来探索这些化合物与GBM受体的结合相互作用。结果:化合物3和5具有明显的抗肿瘤活性,比对照组更有效地降低细胞活力。MTT测定结果证实了其效价。分子对接研究揭示了与GBM受体的强结合相互作用,突出了它们作为抗癌药物的潜力。结论:本研究评价了所合成化合物对人GBM细胞的抑癌活性,其中化合物3和5的抑癌效果最好。吡唑3在高浓度下显著降低细胞活力,而吡唑3和吡唑5的IC50值表明,它们需要更高的剂量才能达到实质性效果。分子对接研究证实了与GBM受体的强结合相互作用,药代动力学特性表明它们可能是抗癌药物。这些结果突出了化合物3和5作为进一步研究的候选物。
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Promising Anticancer Activity of Pyrazole Compounds against Glioblastoma Multiforme: Their Synthesis, In vitro, and Molecular Docking Studies.

Background: Glioblastoma Multiforme (GBM), a highly aggressive and prevalent brain cancer with a higher incidence in males, has limited treatment success due to drug resistance, inadequate targeting and penetration of cancer cells, and an incomplete understanding of its molecular pathways. GBM is a highly aggressive brain cancer with limited treatment options. This study investigates the anticancer potential of synthesized pyrazole compounds against GBM cells.

Methods: A series of pyrazole derivatives were synthesized and tested for their efficacy against GBM using MTT assays. Molecular docking studies were conducted to explore the binding interactions of these compounds with GBM receptors.

Results: Compounds 3 and 5 demonstrated significant anticancer activity, reducing cell viability more effectively than the control group. MTT assay results confirmed their potency. Molecular docking studies revealed strong binding interactions with GBM receptors, highlighting their potential as anticancer agents.

Conclusion: The study evaluated the anticancer activity of synthesized compounds on human GBM cells, with compounds 3 and 5 showing the most promising results. Pyrazole 3 significantly reduced cell viability at high concentrations, while both pyrazoles 3 and 5 required higher doses to achieve substantial effects, as indicated by their IC50 values. Molecular docking studies confirmed strong binding interactions with the GBM receptor, and the pharmacokinetic properties suggest their potential as anticancer agents. These results highlight compounds 3 and 5 as candidates for further investigation.

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来源期刊
Medicinal Chemistry
Medicinal Chemistry 医学-医药化学
CiteScore
4.30
自引率
4.30%
发文量
109
审稿时长
12 months
期刊介绍: Aims & Scope Medicinal Chemistry a peer-reviewed journal, aims to cover all the latest outstanding developments in medicinal chemistry and rational drug design. The journal publishes original research, mini-review articles and guest edited thematic issues covering recent research and developments in the field. Articles are published rapidly by taking full advantage of Internet technology for both the submission and peer review of manuscripts. Medicinal Chemistry is an essential journal for all involved in drug design and discovery.
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