Cancer is one of the leading causes of death. The aim of the present study was to synthesize and investigate the anticancer and antioxidant activities of some 3,5-bis(substituted benzylidene)- 1-ethylpiperidin-4-one analogues (4a-g).

The 3,5-bis(substituted benzylidene)-1-ethylpiperidin-4-one analogues (4a-g) were prepared from the precursor, piperidin-4-one hydrochloride (1). The initial step involved the synthesis of intermediates, 3,5-bis(substituted benzylidene)piperidin-4-one analogues (3a-g) followed by their ethylation with C₂H₅I in acetone and K₂CO₃ to obtain the title compounds (4a-g). The Fourier transform infrared (FTIR), nuclear magnetic resonance (¹H & ¹³C NMR), mass spectrometry and microanalysis were used to characterize the title compounds (4a-g). All the compounds were further evaluated for their anticancer activity by SRB assay and NCI US protocol, while the antioxidant activity was evaluated by DPPH free radical assay. All the title compounds (4a-g) were subjected to molecular docking studies against EGRF tyrosine kinase, a potential target for anticancer agents, to study the possible mode of interaction of our compounds with the molecular target.

The compound 4g showed significant anticancer activity with GI₅₀ of 28.2 μM against MCF-7 (Breast cancer cell line). The antioxidant activity of compound 4g (IC₅₀ = 14.98±0.91 μM) was found to be comparable to the standard drug ascorbic acid. The binding modes of compounds 4a-g against the molecular target EGFR tyrosine kinase were also studied. The structure-activity relationship (SAR) was also studied.

The compound 4g showed significant anticancer activity with GI₅₀ of 28.2 μM against MCF-7 (Breast cancer cell line). The antioxidant activity of the compound, 4g was found to be comparable to the standard drug ascorbic acid, while its anticancer activity was found to be less than that of the standard drug adriamycin.

癌症是导致死亡的主要原因之一。本研究的目的是合成和研究一些 3,5-双（取代亚苄基）-1-乙基哌啶-4-one 类似物 (4a-g) 的抗癌和抗氧化活性。

3,5-双（取代亚苄基）-1-乙基哌啶-4-酮类似物（4a-g）由前体哌啶-4-酮盐酸盐（1）制备。第一步包括合成中间体，3,5-双（取代亚苄基）哌啶-4-酮类似物（3a-g），然后在丙酮和 K ₂ CO ₃中用 C ₂ H ₅ I乙基化，得到标题化合物(4a-g)。傅里叶变换红外 (FTIR)、核磁共振 ( ¹ H & ¹³C NMR）、质谱和微量分析用于表征标题化合物（4a-g）。通过SRB测定和NCI US方案进一步评估所有化合物的抗癌活性，而通过DPPH自由基测定评估抗氧化活性。所有标题化合物 (4a-g) 都进行了针对 EGRF 酪氨酸激酶（抗癌剂的潜在靶标）的分子对接研究，以研究我们的化合物与分子靶标相互作用的可能模式。

化合物4g显示出显着的抗癌活性，对MCF-7（乳腺癌细胞系）的GI ₅₀为28.2 μM。发现化合物 4g (IC ₅₀ = 14.98±0.91 μM)的抗氧化活性与标准药物抗坏血酸相当。还研究了化合物 4a-g 对分子靶标 EGFR 酪氨酸激酶的结合模式。还研究了构效关系（SAR）。

化合物4g显示出显着的抗癌活性，对MCF-7（乳腺癌细胞系）的GI ₅₀为28.2 μM。发现该化合物 4g 的抗氧化活性与标准药物抗坏血酸相当，而其抗癌活性低于标准药物阿霉素。