Akram Muhammad Toseef, Khan Mohsin Abbas, Ahmad Irshad, Ullah Farhat, Khan Muhammad Rizwan, Yasmeen Zarmeena, Ahmad Khalil, Breena Breena
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, 63100, Pakistan.
University College of Conventional Medicine, Faculty of Medicine and Allied Health Sciences, The Islamia University of Bahawalpur, 63100, Pakistan.
Future Med Chem. 2024;16(23):2459-2473. doi: 10.1080/17568919.2024.2408213. Epub 2024 Oct 15.
Breast cancer is the most recurring cancer among females and is being diagnosed as a major cause of death among women. Levosulpiride Schiff base derivatives were synthesized and analyzed by physical and spectral (FTIR, H-NMR, C-NMR) analysis. MTT assay against MCF-7 (human breast cancer cell line), scavenging activity and Molecular docking against receptors 1M17, 3PP0, 3IOK and 4KIK along ADME pharmacokinetic studies were performed. L1 and L3 synthesized derivatives have revealed better percent cell viability and inhibitory concentration (IC) with scavenging activity as of the parent compound. L1, L3 and L9 revealed significant docking scores compared with standard drugs. Most of the derivatives showed strong pharmacokinetic profiles while no drug crossed blood-brain barrier. The newly synthesized L1 and L3 levosulpiride-derived compounds have demonstrated promising anticancer properties against breast cancer cells.
乳腺癌是女性中最易复发的癌症，并且被诊断为女性死亡的主要原因。合成了左舒必利席夫碱衍生物，并通过物理和光谱（傅里叶变换红外光谱、氢核磁共振、碳核磁共振）分析进行了表征。开展了针对MCF-7（人乳腺癌细胞系）的MTT测定、清除活性测定以及针对受体1M17、3PP0、3IOK和4KIK的分子对接，并进行了药物代谢动力学（ADME）研究。合成的衍生物L1和L3显示出比母体化合物更好的细胞活力百分比和抑制浓度（IC）以及清除活性。与标准药物相比，L1、L3和L9显示出显著的对接分数。大多数衍生物表现出良好的药物代谢动力学特征，不过没有药物能够穿过血脑屏障。新合成的源自左舒必利的化合物L1和L3已显示出对乳腺癌细胞有前景的抗癌特性。
