306764-75-0Relevant academic research and scientific papers
Design, synthesis, and structure-activity relationship studies of novel diaryl ether amides as potential antitumor agents
Zheng, Man-Yi,Huang, Zhi-Ning,Yang, Shao-Mei,Han-Liang,Lu-Xu,Wang, Bao-Rui,Wang, Li-Juan,Wang, Hai-Li,Li, Shan-Hua,Li, Fu-Nan
, p. 727 - 736 (2019/05/22)
Sorafenib is a drug that has been verified to be effective on hepatoma cells. Three series of diaryl ethers have been designed and synthesized based on the structure of sorafenib. The 5m compound shows better inhibitory potency against HepG2 cells (IC50 = 1.96 μM) than sorafenib (IC50 = 9.61μM). These results have been verified with MTT assay and colony-forming assay. Moreover, compound 5m exhibits good antitumor activities against PLC/PRF5, HeLa, A549, and HT-29 cell lines. The excellent bioactivity of compound 5m confirms that a single optical conformation is superior to the racemate. A western blotting analysis indicates that compound 5m induces the apoptosis of HepG2 cells by enhancing the protein levels of p21 and Cl-caspase3.
Structure-based design, structure-activity relationship analysis, and antitumor activity of diaryl ether derivatives
Yang, Shao-Mei,Huang, Zhi-Ning,Zhou, Zhong-Shi,Hou, Jin,Zheng, Man-Yi,Wang, Li-Juan,Jiang, Yu,Zhou, Xin-Yi,Chen, Qiu-Yue,Li, Shan-Hua,Li, Fu-Nan
, p. 1761 - 1773 (2015/03/14)
To identify novel therapeutic agents to treat cancer, we synthesized a series of diaryl ether derivatives. Structure-activity relationship studies revealed that the presence of a chlorine or hydroxyl at the para-position on the phenyl ring (5h or 5k) significantly enhanced antitumor activity. Compound 5h had stronger growth inhibitory activity in HepG2, A549, and HT-29 cells than compound 5k, with IC50 values of 2.57, 5.48, and 30.04 μM, respectively. Compound 5h also inhibited the growth of other cells lines, including Hep3B, PLC/PRF5, SMMC-7721, HeLa, and A375, with IC50 values of 2.76, 4.26, 29.66, 18.86, and 10.21 μM, respectively. The antitumor activity of compound 5h was confirmed by a colony forming assay. Further, our results indicated that the antitumor activity of compound 5h may be mediated by enhancing expression of p21 and cl-caspase3, and leading to apoptosis of cancer cells.
