作为潜在化疗药物的新型吡唑类化合物的设计、合成和生物学评价。

IF 3.2 4区 医学 Q3 CHEMISTRY, MEDICINAL Future medicinal chemistry Pub Date : 2024-07-02 Epub Date: 2024-05-20 DOI:10.1080/17568919.2024.2347090
Maiy Y Jaballah, Nooran S Elleboudy, Marwa Sharaky, Khaled A M Abouzid, Mai I Shahin
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引用次数: 0

摘要

目的:设计和合成吡唑类化疗药物。材料与方法:合成了一系列新型二苯基吡唑-查尔酮衍生物,并使用 HSF 正常细胞系评估了它们对 14 种癌症细胞系的细胞毒活性、对 MRSA 和大肠杆菌的抗菌活性及其安全性。结果与结论:大多数化合物对 HNO-97 具有中度到显著的抗癌活性,选择性抑制率高(>80%),同时对正常细胞无毒。化合物 6b 和 6d 是最有效的同系物,IC50 分别为 10 和 10.56 μM。合成的化合物表现出中等至强效的抗菌活性。有趣的是,化合物 6d 对 MRSA 的最低抑制浓度为 15.7 μg/ml;对大肠杆菌的最低抑制浓度为 7.8 μg/ml。
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Design, synthesis and biological evaluation of novel pyrazole-based compounds as potential chemotherapeutic agents.

Aim: Design and synthesis of pyrazole-based chemotherapeutic agents. Materials & methods: A series of novel diphenyl pyrazole-chalcone derivatives were synthesized and assessed for their cytotoxic activities against 14 cancer cell lines and their antimicrobial activities against MRSA and Escherichia coli along with their safety using HSF normal cell line. Results & conclusion: Majority of the compounds showed moderate-to-significant anticancer activity with selective high percentage inhibition (>80%) against HNO-97 while being nontoxic toward normal cells. Compounds 6b and 6d were the most potent congeners with IC50 of 10 and 10.56 μM respectively. The synthesized compounds exhibited moderate to potent antimicrobial activities. Interestingly, compound 6d exhibited a minimum inhibitory concentration of 15.7 μg/ml against MRSA; and a minimum inhibitory concentration of 7.8 μg/ml versus E. coli.

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来源期刊
Future medicinal chemistry
Future medicinal chemistry CHEMISTRY, MEDICINAL-
CiteScore
5.80
自引率
2.40%
发文量
118
审稿时长
4-8 weeks
期刊介绍: Future Medicinal Chemistry offers a forum for the rapid publication of original research and critical reviews of the latest milestones in the field. Strong emphasis is placed on ensuring that the journal stimulates awareness of issues that are anticipated to play an increasingly central role in influencing the future direction of pharmaceutical chemistry. Where relevant, contributions are also actively encouraged on areas as diverse as biotechnology, enzymology, green chemistry, genomics, immunology, materials science, neglected diseases and orphan drugs, pharmacogenomics, proteomics and toxicology.
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