作为抗癌剂的异噁唑并噁唑-4-基-1-(吡啶-4-基)-1H-吡唑的合理设计、合成和生物学评价

IF 2.218 Q2 Chemistry Chemical Data Collections Pub Date : 2024-08-01 DOI:10.1016/j.cdc.2024.101146

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引用次数: 0

摘要

我们开发了一个新的异噁唑骨架库，其中含有噁唑-4-基）-1-(吡啶-4-基)-1H-吡唑衍生物（9a-j）。此外，还采用 MTT 法检测了新化合物（9a-j）对四种人类癌细胞系（如乳腺癌（MCF-7）、肺癌（A549）、前列腺癌（DU-145）和乳腺癌（MDA-MB-231））的生物活性，并以依托泊苷作为候选药物参考。结果以 IC50 µM 表示。大多数受试化合物对所有细胞系都显示出良好至中等程度的活性。其中，5 种衍生物 9a、9b、9c、9d 和 9e 具有更强的活性。其中，化合物 9b 显示出了显著的活性。

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Rational design, synthesis and biological evaluation of Isoxazole incorporated oxazol-4-yl-1-(pyridin-4-yl)-1H-pyrazole as anticancer agents

We have developed a new library of isoxazole skeleton having oxazol-4-yl)-1-(pyridin-4-yl)-1H-pyrazole derivatives (9a-j). Further, the biological activity of newly derived compounds (9a-j) was examined against four types of human cancer cell lines like breast cancer (MCF-7), lung cancer (A549), prostate cancer (DU-145) and breast cancer (MDA-MB-231) by employing of MTT assay, and etoposide used as reference drug candidate. The results were expressed with IC₅₀ µM. Most of the tested compounds displayed good to moderate activities on all cell lines. Among them, five derivatives 9a, 9b, 9c, 9d and 9e were possessed more potent activity. Principally, one of the compound 9b showed remarkable activity.

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来源期刊

Chemical Data Collections Chemistry-Chemistry (all)

CiteScore

6.10

自引率

0.00%

发文量

169

审稿时长

24 days

期刊介绍： Chemical Data Collections (CDC) provides a publication outlet for the increasing need to make research material and data easy to share and re-use. Publication of research data with CDC will allow scientists to: -Make their data easy to find and access -Benefit from the fast publication process -Contribute to proper data citation and attribution -Publish their intermediate and null/negative results -Receive recognition for the work that does not fit traditional article format. The research data will be published as ''data articles'' that support fast and easy submission and quick peer-review processes. Data articles introduced by CDC are short self-contained publications about research materials and data. They must provide the scientific context of the described work and contain the following elements: a title, list of authors (plus affiliations), abstract, keywords, graphical abstract, metadata table, main text and at least three references. The journal welcomes submissions focusing on (but not limited to) the following categories of research output: spectral data, syntheses, crystallographic data, computational simulations, molecular dynamics and models, physicochemical data, etc.