Advances in the study of structural modifications of multi-target anticancer drug sorafenib.
- Author:
Jian-Wen YAO
1
;
Wei SUN
;
Jing CHEN
;
Wen-Fang XU
Author Information
1. School of Pharmaceutical Sciences, Shandong University Jinan 250012, China.
- Publication Type:Journal Article
- MeSH:
Animals;
Antineoplastic Agents;
chemical synthesis;
chemistry;
Cell Line, Tumor;
Humans;
Molecular Structure;
Neoplasms;
drug therapy;
pathology;
Neovascularization, Pathologic;
prevention & control;
Niacinamide;
analogs & derivatives;
chemical synthesis;
chemistry;
Phenylurea Compounds;
chemical synthesis;
chemistry;
Protein Kinase Inhibitors;
chemical synthesis;
chemistry;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2012;47(9):1111-1119
- CountryChina
- Language:Chinese
-
Abstract:
Sorafenib, the first oral multikinase inhibitor, can inhibit several kinases involved in tumor proliferation and angiogenesis including Raf, VEGFR, PDGFR, kit and so on. Due to the advantages of multi-mechanisms, broad-spectrum anticancer potency, and well-tolerated results in combination trials, more and more researchers have focused on the optimization of sorafenib in order to develop novel multi-targeted anticancer drugs. The present paper reviews the development of modification of sorafenib in recent years from two aspects: bio-isosterism and scaffold hopping. The structure-activity relationship (SAR) of these compounds is also summarized.