Zhang Qijing, Dong Jinyun, Cui Jiahua, Huang Guang, Meng Qingqing, Li Shaoshun
School of Pharmacy, Shanghai Jiao Tong University.
Chem Pharm Bull (Tokyo). 2018;66(6):612-619. doi: 10.1248/cpb.c18-00013.
In an effort to develop potent and selective antitumor agents, a series of 1,4-naphthoquinone oxime derivatives were designed and synthesized. The cytotoxicity of these compounds were evaluated against five human cancer cell lines (colorectal cancer cell: HCT-15, breast cancer cell: MDA-MB-231, liver cancer cell: BEL-7402, colorectal cancer cell: HCT-116 and ovarian cancer cell: A2780) in vitro. Among them, compound 14 was found to be the most potent cytotoxic compound against three cell lines (MDA-MB-231, BEL-7402 and A2780) with IC values of 0.66±0.05, 5.11±0.12 and 8.26±0.22 µM, respectively. Additionally, the length of the side chains and the position of the substituent may also affect the cytotoxic activity of the naphthoquinone oxime derivatives. In general, compound 14 effectively inhibited breast cancer cell proliferation and may become a promising anticancer agent.
为了开发高效且具选择性的抗肿瘤药物，设计并合成了一系列1,4-萘醌肟衍生物。在体外对这些化合物针对五种人类癌细胞系（结肠癌细胞：HCT-15、乳腺癌细胞：MDA-MB-231、肝癌细胞：BEL-7402、结肠癌细胞：HCT-116和卵巢癌细胞：A2780）的细胞毒性进行了评估。其中，化合物14被发现是针对三种细胞系（MDA-MB-231、BEL-7402和A2780）最具细胞毒性的化合物，其IC值分别为0.66±0.05、5.11±0.12和8.26±0.22 μM。此外，侧链长度和取代基位置也可能影响萘醌肟衍生物的细胞毒性活性。总体而言，化合物14有效抑制乳腺癌细胞增殖，可能成为一种有前景的抗癌药物。
