Design, synthesis and biological evaluation of aryl chalcone derivatives of pyridine-benzoxazole-pyimidine-oxazole as anticancer agents

IF 2.5 Q2 CHEMISTRY, MULTIDISCIPLINARY

Results in Chemistry Pub Date : 2025-05-14 DOI:10.1016/j.rechem.2025.102359

Abdulrhman Alsayari , S. Tasqeeruddin , Shaheen Sultana , Laxminarayana Eppakayala

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Abstract

A new library of aryl chalcone derivatives of pyridine-benzoxazole-pyimidine-oxazole (27a-j) and their chemical structures were confirmed by analytical data. Further, all the newly synthesized compounds (27a-j) were evaluated for their anticancer applications against human cancer cell lines by the MTT method. Here, the chemotherapeutic agent etoposide is used as a positive control. The obtained results were compared with etoposide. Most of the screened compounds displayed remarkable anticancer activity on all cell lines. Among them, five compounds exhibited more potent anticancer activity as compared to the positive control. Mainly, one compound, 27j, displayed superior activity on four cell lines. Furthermore, all the compounds displayed selective cytotoxicity against cancer cells but not against normal Vero cells (IC50 ≥19 μM), supporting the design method as a selective anticancer agents.

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吡啶-苯并恶唑-嘧啶-恶唑芳基查尔酮类抗癌药物的设计、合成及生物学评价

用分析数据确定了一个新的吡啶-苯并恶唑-嘧啶-恶唑（27a-j）芳基查尔酮衍生物文库及其化学结构。此外，所有新合成的化合物（27a-j）通过MTT方法对人类癌细胞系的抗癌应用进行了评价。在这里，化疗药物依托泊苷被用作阳性对照。所得结果与依托泊苷进行了比较。大多数筛选的化合物对所有细胞系都显示出显著的抗癌活性。其中，有5种化合物的抗癌活性比阳性对照更强。其中化合物27j在4种细胞系中表现出较强的活性。此外，所有化合物对癌细胞均表现出选择性细胞毒性，但对正常Vero细胞不表现出选择性细胞毒性（IC50≥19 μM），支持该设计方法作为选择性抗癌药物。

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