Synthesis and in vitro cytotoxic activities of sorafenib derivatives.
- Author:
Ke WANG
;
Yan LI
;
Li-Jing ZHANG
;
Han-Ze YANG
;
Xiao-Guang CHEN
;
Zhi-Qiang FENG
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Cell Line, Tumor;
Cell Proliferation;
drug effects;
Humans;
Inhibitory Concentration 50;
Molecular Structure;
Niacinamide;
analogs & derivatives;
chemical synthesis;
chemistry;
pharmacology;
Phenylurea Compounds;
chemical synthesis;
chemistry;
pharmacology;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2014;49(5):639-643
- CountryChina
- Language:Chinese
-
Abstract:
A series of novel sorafenib analogues were designed and synthesized. The cytotoxic activities of these compounds were tested in four tumor cell lines. Some of the compounds showed potent antiproliferative activity against the tested cell lines with IC50 = 4-20 micromol x L(-1). Some compounds demonstrated competitive antiproliferative activities to sorafenib against tested cancer cell lines. Among them, compound 7c demonstrated significant inhibitory activities on ACHN, HCT116 and MDA-MB-231 cell lines with IC50 values of 9.01, 4.97, 6.61 micromol x L(-1), respectively.