Li Jing, Sui Yun-Peng, Xin Jia-Jia, Du Xin-Liang, Li Jiang-Tao, Huo Hai-Ru, Ma Hai, Wang Wei-Hao, Zhou Hai-Yu, Zhan Hong-Dan, Wang Zhu-Ju, Li Chun, Sui Feng, Li Xia
School of Chemical Engineering, The Key Laboratory for Surface Engineering and Remanufacturing in Shaanxi Province, Xi'an University, Xi'an 710065, China.
Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China; Beijing Chao-Yang Hospital, Capital Medical University, Beijing 100020, China.
Bioorg Med Chem Lett. 2015 Dec 1;25(23):5520-3. doi: 10.1016/j.bmcl.2015.10.063. Epub 2015 Oct 23.
Two series of biscoumarin (1-3) and dihydropyran (4-12) derivatives were successfully synthesized as new antitumor and antibacterial agents. The molecular structures of four representative compounds 2, 4, 7 and 10 were confirmed by single crystal X-ray diffraction study. The synthesized compounds (1-12) were evaluated for their antitumor activities against human intestinal epithelial adenocarcinoma cell line (HuTu80), mammary adenocarcinoma cell line (4T1) and pancreatic cancer cell line (PANC1) and antibacterial activities against one drug-sensitive Staphylococcus aureus (S. aureus ATCC 29213) strain and three MRSA strains (MRSA XJ 75302, Mu50, USA 300 LAC). The further mechanism study demonstrated that the most potent compound 1 could obviously inhibit the proliferation of cancer cells via the mechanism to induce apoptosis.
成功合成了两个系列的双香豆素（1-3）和二氢吡喃（4-12）衍生物作为新型抗肿瘤和抗菌剂。通过单晶X射线衍射研究确定了四种代表性化合物2、4、7和10的分子结构。对合成的化合物（1-12）进行了评估，考察它们对人肠上皮腺癌细胞系（HuTu80）、乳腺腺癌细胞系（4T1）和胰腺癌细胞系（PANC1）的抗肿瘤活性，以及对一株药敏金黄色葡萄球菌（金黄色葡萄球菌ATCC 29213）和三株耐甲氧西林金黄色葡萄球菌（MRSA XJ 75302、Mu50、USA 300 LAC）的抗菌活性。进一步的机制研究表明，最有效的化合物1可通过诱导凋亡的机制明显抑制癌细胞的增殖。
