Background: The era of drug discovery suggested the designing of “hybrid drugs,” which acquired recognition in the field of medicinal chemistry due to its influential role in preserving different health challenges.

Objective: A new series of chalcone derivatives 4a-4i, bearing isoxazole moieties, were designed and synthesized with microwave irradiation, which were biologically evaluated for their activity on NCI- 60 cell-lines to check efficacy in anti-cytotoxic effect.

Methods: The required diverse acetophenone molecule was prepared by chloro-amine coupling using lansoprazole (lanso chloro) drug intermediate, i.e., 4-(2,2,2-trifluoroethoxy)-2-(chloromethyl)-3- methylpyridine engaged in the reaction with various aryl aldehydes (2a-2i) in the primary media gave fluoro contained chalcone (3a-3i). The desired isoxazoles (4a-4i) were synthesized by MW (microwave irradiation) based reaction using hydroxylamine for cyclization purposes.

Results: The espoused scheme resulted in good yields of a new set of isoxazole-chalcone conjugates with potent cytotoxic activity, which were found in compounds 4h and 4i against the Leukemia RPMI-8226 (With GI₅₀ Values ≈ -10 μg/ml) cancer cell line and the Non-Small Cell Lung Cancer HOP-92 (With GI₅₀ Values ≈ -25 μg/ml) cancer cell line.

Conclusion: The optimization of the reaction indicated that the MW based reaction progress was an efficient and time-saving process for the course of isoxazole synthesis. An anticancer study shows that compounds 4h demonstrated significant anticancer activity.

背景：药物发现时代提出了“混合药物”的设计，由于其在应对不同健康挑战方面的重要作用而在药物化学领域获得了认可。

目的：设计并利用微波辐射合成了一系列带有异恶唑部分的新查耳酮衍生物 4a-4i，对它们对 NCI-60 细胞系的活性进行生物学评估，以检查其抗细胞毒作用的功效。

方法：使用兰索拉唑（lanso chloro）药物中间体，即4-（2,2,2-三氟乙氧基）-2-（氯甲基）-3-甲基吡啶，通过氯胺偶联制备所需的多种苯乙酮分子。与初级介质中的各种芳基醛 (2a-2i) 反应得到含氟的查耳酮 (3a-3i)。所需的异恶唑 (4a-4i) 是通过基于 MW（微波辐射）的反应合成的，使用羟胺进行环化。

结果：支持的方案产生了一组具有有效细胞毒性活性的新异恶唑-查尔酮缀合物的良好产量，这些化合物在化合物 4h 和 4i 中被发现对白血病 RPMI-8226（GI ₅₀值≈ -10 μg/ml）癌症细胞系和非小细胞肺癌 HOP-92（GI ₅₀值 ≈ -25 μg/ml）癌细胞系。

结论：反应的优化表明，基于分子量的反应进程是异恶唑合成过程中一种高效、省时的过程。一项抗癌研究表明，化合物 4h 显示出显着的抗癌活性。