Zhou Wu-Xi, Cao Jia-Qing, Wang Xu-De, Guo Jun-Hui, Zhao Yu-Qing
Department of Traditional Chinese Medicine Chemical, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Department of Traditional Chinese Medicine Chemical, Shenyang Pharmaceutical University, Shenyang 110016, PR China; Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
Bioorg Med Chem Lett. 2017 Feb 15;27(4):1076-1080. doi: 10.1016/j.bmcl.2016.12.048. Epub 2016 Dec 21.
In the search for new anti-tumor agents with higher potency than our previously identified compound 1 (25-OH-PPD, 25-hydroxyprotopanaxadiol), 12 novel sulfamic and succinic acid derivatives that could improve water solubility and contribute to good drug potency and pharmacokinetic profiles were designed and synthesized. Their in vitro anti-tumor activities in MCF-7, A-549, HCT-116, and BGC-823 cell lines and one normal cell line were tested by standard MTT assay. Results showed that compared with compound 1, compounds 2, 3, and 7 exhibited higher cytotoxic activity on A-549 and BGC-823 cell lines, together with lower toxicity in the normal cell. In particular, compound 2 exhibited the best anti-tumor activity in the in vitro assays, which may provide valuable data for the research and development of new anti-tumor agents.
为了寻找比我们之前鉴定的化合物1（25-羟基原人参二醇，25-OH-PPD）效力更高的新型抗肿瘤药物，设计并合成了12种新型氨基磺酸和琥珀酸衍生物，这些衍生物可以提高水溶性，并有助于获得良好的药物效力和药代动力学特征。通过标准MTT法检测了它们在MCF-7、A-549、HCT-116和BGC-823细胞系以及一种正常细胞系中的体外抗肿瘤活性。结果表明，与化合物1相比，化合物2、3和7对A-549和BGC-823细胞系表现出更高的细胞毒性活性，同时对正常细胞的毒性更低。特别是，化合物2在体外试验中表现出最佳的抗肿瘤活性，这可能为新型抗肿瘤药物的研发提供有价值的数据。
