Citation: Ke Wang, Yan Li, Li-Jing Zhang, Xiao-Guang Chen, Zhi-Qiang Feng. Synthesis and in vitro cytotoxic activities of sorafenib derivatives[J]. Chinese Chemical Letters, ;2014, 25(05): 702-704. doi: 10.1016/j.cclet.2014.03.020 shu

Synthesis and in vitro cytotoxic activities of sorafenib derivatives

1.
a State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China;
2.
b Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China

Corresponding author: Zhi-Qiang Feng,
Received Date: 21 January 2014
Available Online: 28 February 2014
Fund Project: We gratefully acknowledge the generous support provided by the National S&T Major Special Project on Major New Drug Innovation (No. 2012ZX09103-101-019). (No. 2012ZX09103-101-019)

A series of novel sorafenib derivatives have been designed and synthesized. The cytotoxic activities of these compounds were tested in three tumor cell lines. Most of the compounds showed potent antiproliferative activity against the tested cell lines with IC₅₀ = 0-20 μmol/L. Some compounds demonstrated competitive antiproliferative activities to sorafenib against all three cancer cell lines. Among them, compound 5g demonstrated significant inhibitory activity against A549, ACHN and MDAMB- 231 cell lines with IC₅₀ values of 1.29, 1.99, 3.11 μmol/L, respectively.
- Sorafenib,
- Antiproliferative activity,
- A549,
- ACHN,
- MDA-MB-231
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沈阳化工大学材料科学与工程学院沈阳 110142