Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase

Design and synthesis of VEGFR-2 tyrosine kinase inhibitors as potential anticancer agents by virtual based screening

“…The QikProp 3.2 is used to analyze drug likeness (Lipinski's rule of ve), and the results are given in Table 6. It was found that all the synthesized compounds comply with these rules, except for 28,31,32,44,61,70 Following are some of the predictions and the reasons that probably caused this opening and closing of the ring. The substituents have a dominant bearing on the reactivity of the benzoxazinone carbonyl and the electronic contribution, in particular, of the ring substituents seems to dominate.…”

Design, synthesis, and bioactivity evaluation of antitumor sorafenib analogues

“…The design of protein kinase inhibitors that can interfere with the cell signal transduction pathway has been used in the search for disease drug treatments. [42][43][44][45] Agents that act on the signal transduction pathway mechanism in tumors include protein kinase inhibitors and proteasome inhibitors. Protein kinase inhibitors can be divided into Bcr-Abl protein kinase inhibitors, epidermal growth factor receptor tyrosine kinase inhibitors, and multiple kinase target inhibitors.…”

Synthesis and Biological Evaluation of Urea Derivatives of Combretastatins as Anticancer Agents

“…Aryl urea moiety was a important functional group in numerous natural products and drug intermediates 12 and building blocks for various heterocyclic compounds 13,14 . Some of the aryl urea derivatives showed a numerous biological activities such as antitumor 15 , inhibit the polymerization of tubulin 16 anti-inflammatory 17 , antimalarial 18 and antidiabetic 19 , antituberculosis, antibacterial and RESEARCH ARTICLE anticonvulsant [20][21][22] antibiotic 23 and hypoglycemic activities 24 . Sorafenib (3) was a bi-aryl urea ( Figure 1) developed by Bayer, is currently used for the treatment of hepatocellular carcinoma (HCC) 25 , renal cell carcinoma (RCC) 26 .…”