Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Yenimahalle, 06560, Ankara, Turkey.
Department of Biochemistry, Faculty of Pharmacy, Ankara University, Yenimahalle, 06560, Ankara, Turkey.
Naunyn Schmiedebergs Arch Pharmacol. 2024 May;397(5):3169-3177. doi: 10.1007/s00210-023-02799-6. Epub 2023 Oct 28.
In this study, the anticancer activities of some pyrrolopyrimidine derivatives were evaluated. Compound 3 is the most cytotoxic compound on MCF-7 cancer cells with an IC value of 23.42 µM. Also, compound 3 induced apoptosis and the ROS(+) cell population in MCF-7 cells. Moreover, it significantly reduced MMP-9 activity, having 42.16 ± 5.10% and 58.28 ± 1.96% inhibitory activities at 10 µM and 50 µM concentrations, respectively. Molecular docking results supported the activity, showing key hydrogen bonds with the binding site of MMP-9. Therefore, compound 3 might be a lead compound for the development of potent MMP-9 inhibitors.
在这项研究中，评估了一些吡咯并嘧啶衍生物的抗癌活性。化合物 3 对 MCF-7 癌细胞的细胞毒性最强，IC 值为 23.42µM。此外，化合物 3 诱导 MCF-7 细胞凋亡和 ROS(+)细胞群体。此外，它还显著降低了 MMP-9 的活性，在 10µM 和 50µM 浓度下，分别具有 42.16±5.10%和 58.28±1.96%的抑制活性。分子对接结果支持了这一活性，显示出与 MMP-9 结合位点的关键氢键。因此，化合物 3 可能是开发强效 MMP-9 抑制剂的先导化合物。
