Advances in the study of structural modifications of multi-target anticancer drug sorafenib / 药学学报

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.