It’s only fair to share… The Food and Drug Administration (FDA) has approved several quinazoline derivatives for clinical use as anticancer drugs. These include gefitinib, erlotinib, lapatinib, afatinib, and vandetanib (Fig.1) [43]. Gefitinib (Iressa®) was approved by the FDA in 2003 for the treatment of locally advanced or metastatic non-small-cell lung cancer (NSCLC) in …
Tag «anticancer agents»
2-Arylideneimidazo[1,2-a]pyridinones as Topoisomerase IIα-Inhibiting Anticancer Agents
It’s only fair to share… Scaffold-hopping of bioactive natural product aurones has been studied for the first time. 2-Arylideneimidazo[1,2-a]pyridinones as potential topoisomerase IIα (hTopoIIα)-targeting anticancer compounds were considered. A multifunctional activator, polyphosphoric acid, enabled to realize a cascade reaction of 2-aminopyridine with 2,3-epoxyesters toward synthesis of 2-arylideneimidazo[1,2-a]pyridinones. Most of the compounds exhibited hTopoIIα-selective poison activity …