| Literature DB >> 24747188 |
Maosheng Wan1, Linyan Xu2, Li Hua3, Ailing Li3, Shuqing Li3, Wenjing Lu1, Yue Pang1, Chengbo Cao4, Xiangguo Liu2, Peifu Jiao5.
Abstract
A series of novel isoxazolyl chalcones were synthesized and evaluated for their activities in vitro against four types of human non-small cell lung cancer cells, including H1792, H157, A549 and Calu-1 cells. The preliminary biological screening showed that compounds 5d and 5f-i exhibited significant cytotoxicity, particularly, compounds 5f and 5h were identified as the most potent anticancer agents with IC50 values 1.35-2.07 μM and 7.27-11.07 μM against H175, A549 and Calu-1 cell lines, respectively. Compounds 5f-i could induce apoptosis in A549 cells by death receptor 5 (DR5) mediated extrinsicpathways. The preliminary structure-activity relationship study showed that compounds bearing electron withdrawing groups (EWG) at the 2-position of the phenyl ring in Ar group were more effective than those with EWG at 4-position. These results further demonstrated that the scaffolds designed in this work might lead to the discovery of novel anti-lung cancer agents.Entities:
Keywords: Apoptosis; Death receptor 5; Human non-small cell lung cancer cells; Isoxazolyl chalcones; Synthesis
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Year: 2014 PMID： 24747188 DOI： 10.1016/j.bioorg.2014.03.004
Source DB: PubMed Journal: Bioorg Chem ISSN： 0045-2068 Impact factor: 5.275