PDF(Pubmed)
Abstract：
In this study we presented a novel series of NNO tridentate ligands generating imino, amido and oxo donor pocket for Pd(II) coordination. All the compounds were meticulously characterized by elemental analysis and advanced spectroscopic techniques, including FTIR, proton and carbon NMR. The synthesized compounds underwent rigorous evaluation for their potential as anti-cancer agents, utilizing the aggressive breast cancer cell lines MDA-MB (ATCC) and MCF-7 as a crucial model for assessing growth inhibition in cancer cells. Remarkably, the MTT assay unveiled the robust anti-cancer activity for all palladium complexes against MDA-MB-231 and MCF-7 cells. Particularly, complex [Pd(L1)(CH3CN)] exhibited exceptional potency with an IC50 value of 25.50 ± 0.30 µM (MDA-MB-231) and 20.76 ± 0.30 µM (MCF-7), compared to respective 27.00 ± 0.80 µM and 24.10 ± 0.80 µM for cisplatin, underscoring its promising therapeutic potential. Furthermore, to elucidate the mechanistic basis for the anti-cancer effects, molecular docking studies on tyrosine kinases, an integral target in cancer research, were carried out. The outcome of these investigations further substantiated the remarkable anticancer properties inherent to these innovative compounds. This research offers a compelling perspective on the development of potent anti-cancer agents rooted in the synergy between ligands and Pd(II) complexes and presenting a promising avenue for future cancer therapy endeavors.
摘要：
在这项研究中，我们提出了一系列产生亚氨基的NNO三齿配体，酰胺基和氧代供体口袋用于Pd(II)配位。所有化合物都经过元素分析和先进的光谱技术精心表征，包括FTIR,质子和碳核磁共振。合成的化合物经过严格的评估，作为抗癌药物的潜力，利用侵袭性乳腺癌细胞系MDA-MB（ATCC）和MCF-7作为评估癌细胞生长抑制的关键模型。值得注意的是,MTT分析揭示了所有钯复合物对MDA-MB-231和MCF-7细胞的强大抗癌活性。特别是,复合物[Pd（L1）（CH3CN）]表现出优异的效力，IC50值为25.50±0.30µM（MDA-MB-231）和20.76±0.30µM（MCF-7），与顺铂各自的27.00±0.80µM和24.10±0.80µM相比，强调了其有前途的治疗潜力。此外，为了阐明抗癌作用的机理基础，酪氨酸激酶的分子对接研究，癌症研究中不可或缺的目标，进行了。这些研究的结果进一步证实了这些创新化合物固有的显著抗癌特性。这项研究为根植于配体和Pd（II）复合物之间的协同作用的有效抗癌剂的开发提供了令人信服的观点，并为未来的癌症治疗努力提供了有希望的途径。
