在未来的几十年里，全球癌症的发病率和死亡率预计将上升，其中结直肠癌和前列腺癌是最常见的癌症类型。尽管分子靶向治疗取得了进步，但铂类化疗仍然是治疗的基石，特别是对于结直肠癌和前列腺癌，奥沙利铂和顺铂由于其 DNA 靶向能力而极其有效。在我们追求毒性更低、更有效的新型铂基化疗药物的过程中，我们探索了奥沙利铂中使用的二氨基环己烷环的铂结合基团与稳定的氨基嘧啶半姜黄素部分的组合。这种新的衍生物在生理条件下表现出更高的稳定性，并在水介质中增加溶解度，显示出对结直肠和前列腺细胞的细胞增殖的有希望的作用。我们在此报告了新衍生物 [(1R,2R)-N1-(3-(4-((E)-2-(2-Amino-6-methylpyrimidin-4-yl)) 的完整合成和溶液中的化学表征乙烯基)-2-甲氧基苯氧基)丙基)环己烷-1,2-二胺](MPYD)。我们的分析包括检查其酸碱平衡、形态和生理条件下的稳定性。通过核磁共振波谱研究了 Pt(II) 配合物的合成和原位形成，同时采用密度泛函理论计算来阐明溶液中的化学结构。生物活性结果是通过对不同结直肠和前列腺细胞系（HCT116、HT29、PC3 和 LNCaP）进行细胞活力测定而获得的。版权所有 © 2024。由 Elsevier Inc. 出版。

In the upcoming decades, the incidence and mortality rates of cancer are expected to rise globally, with colorectal and prostate cancers among the most prevalent types. Despite advancements in molecular targeted therapy, platinum-based chemotherapies remain the cornerstone of treatment, especially for colorectal and prostate cancer, with oxaliplatin and cisplatin being extremely effective due to their DNA-targeting capabilities. In our pursuit of new platinum-based chemotherapeutics that are potentially less toxic and more effective, we have explored the combination of the Pt-binding groups of the diaminocyclohexane ring used in oxaliplatin, with the stable amino-pyrimidine hemicurcumin moiety. This new derivative exhibit improved stability in physiological conditions and increased solubility in aqueous media, demonstrating promising effects on cell proliferation of both colorectal and prostate cells. We report herein the complete synthesis and chemical characterization in solution of the new derivative [(1R,2R)-N1-(3-(4-((E)-2-(2-Amino-6-methylpyrimidin-4-yl)vinyl)-2-methoxyphenoxy) propyl) cyclohexane-1,2-diamine] (MPYD). Our analysis includes an examination of its acid-base equilibria, speciation and stability in physiological conditions. The synthesis and in situ formation of Pt(II) complexes were investigated by nuclear magnetic resonance spectroscopy, while density functional theory calculations were employed to elucidate the chemical structure in solution. Results on the biological activity were obtained through cell viability assays on different colorectal and prostate cell lines (HCT116, HT29, PC3 and LNCaP).Copyright © 2024. Published by Elsevier Inc.