New pyrano-pyridine conjugates as potential anticancer agents: design, synthesis and computational studies.

IF 3.2 4区医学 Q3 CHEMISTRY, MEDICINAL

Future medicinal chemistry Pub Date : 2024-11-24 DOI:10.1080/17568919.2024.2431475

Aladdin M Srour, Eman S Nossier, Najla A Altwaijry, Safeya M Mousa, Hanem M Awad, Heba S A Elzahabi

引用次数: 0

Abstract

Aim: New pyrano[3,2-c]pyridine 4a-h, 5-8 and pyrano[2,3-d]pyrimidin 9a,b series were designed and chemically synthesized.

Methodology: Using the standard drug doxorubicin, the novel chemical entities have been assessed in vitro as potential anticancer prospects on cell lines from liver, breast, colon, and lung cancer along with examining their inhibitory behaviors upon both EGFR and VEGFR-2 kinases.

Results & conclusion: Compared to erlotinib (IC₅₀ = 0.18 µM), compounds 8a and 8b demonstrated the highest anticancer activity with IC₅₀ Values 0.23 and 0.15 µM, respectively). Further, derivative 8a illustrated encouraging inhibitory characteristics against EGFR and VEGFR-2 (IC₅₀ = 1.21 and 2.65 μM, respectively). A computational study was used to estimate the physicochemical and pharmacokinetic properties to afford insightful information about the newly synthesized agents.

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作为潜在抗癌剂的新吡喃吡啶共轭物：设计、合成和计算研究。

目的：设计并化学合成了新的吡喃并[3,2-c]吡啶 4a-h、5-8 和吡喃并[2,3-d]嘧啶 9a、b 系列：方法：使用标准药物多柔比星，对新型化学实体进行体外评估，以确定其对肝癌、乳腺癌、结肠癌和肺癌细胞系的潜在抗癌前景，同时考察其对表皮生长因子受体（EGFR）和血管内皮生长因子受体（VEGFR）-2 激酶的抑制行为：与厄洛替尼（IC50 = 0.18 µM）相比，化合物 8a 和 8b 的抗癌活性最高，IC50 值分别为 0.23 和 0.15 µM）。此外，衍生物 8a 对表皮生长因子受体（EGFR）和血管内皮生长因子受体（VEGFR）-2 具有令人鼓舞的抑制特性（IC50 值分别为 1.21 和 2.65 µM）。计算研究用于估算这些新合成制剂的物理化学和药代动力学特性，以提供有关这些制剂的深入信息。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

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.