期刊
CHEMICAL & PHARMACEUTICAL BULLETIN
卷 61, 期 1, 页码 50-58出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.c12-00812
关键词
qunioline; sulfonamide; anticancer activity
资金
- National Plan for Science and Technology Program, King Saud University [10-MED-1223-02]
- King Abdulaziz City for Science and Technology, Riyadh, Saudi Arabia
Based on the reported anticancer activity of quinolines, a new series of 7-chloroquinoline derivatives bearing the biologically active benzenesulfonamide moiety 2-17 and 19-25 were synthesized starting with 4,7-dichloroquinolne 1. Compound 17 was the most active compound with IC50 value 64.41, 75.05 and 30.71 mu M compared with Doxorubicin as reference drug with IC50 values 82.53, 88.32 and 73.72 mu M on breast cancer cells, skin cancer cells and neuroblastoma, respectively. All the synthesized compounds were evaluated for their in vitro anticancer activity on breast cancer cells, skin cancer cells and neuroblastoma cells. Most of the synthesized compounds showed moderate activity. In order to suggest the mechanism of action for their cytotoxic activity, molecular docking for all synthesized compounds was done on the active site of phosphoinositide kinase (PI3K) and good results were obtained.
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