Yang Jia-qiang, Zeng Fa-kun, Yang Xuan, Li Peng
Yao Xue Xue Bao. 2016 Jul;51(7):1105-9.
In search of effective anticancer agents, fifteen new phosphonate derivatives were designed and synthesized. Their structures were clearly established by elemental analysis, IR, (1)H NMR and (13)C NMR, and their antitumor activities were evaluated by MTT assay. Preliminary results in bioactivity tests indicated that some title compounds exhibited better activity. Among the active compounds, compounds 4e, 4n had better inhibition effect on A-549 cells growth with IC(50) values of 8.7 ± 0.8, 8.2 ± 1.0 μmol·L(-1), the IC(50) values of compound 4c was 9.8 ± 0.9 μmol·L(-1) against SGC-7901 cells and compounds 4l, 4n exhibited more potent activities against EC-109 with IC(50) values of 9.5 ± 0.6, 9.4 ± 0.5 μmol·L(-1).
为寻找有效的抗癌药物，设计并合成了15种新型膦酸酯衍生物。通过元素分析、红外光谱、氢核磁共振谱和碳核磁共振谱明确了它们的结构，并采用MTT法评估了它们的抗肿瘤活性。生物活性测试的初步结果表明，一些目标化合物表现出较好的活性。在活性化合物中，化合物4e、4n对A-549细胞生长的抑制作用较好，IC50值分别为8.7±0.8、8.2±1.0 μmol·L-1；化合物4c对SGC-7901细胞的IC50值为9.8±0.9 μmol·L-1；化合物4l、4n对EC-109表现出更强的活性，IC50值分别为9.5±0.6、9.4±0.5 μmol·L-1。
