Syntheses of 4-(indole-3-yl)quinazolines – A new class of epidermal growth factor receptor tyrosine kinase inhibitors

EGFR tyrosine kinase targeted compounds: synthesis, docking study, and in vitro antitumor activity of some new quinazoline and benzo[d]isothiazole derivatives

“…In last decade, 4-anilinoquinazolines have emerged as a versatile template for inhibition of a diverse range of receptor tyrosine kinases (Szczepankiewicz et al, 2000;Tobe et al, 2003). The most widely studied of these are the inhibitors of the epidermal growth factor receptor (EGFR) tyrosine kinase and that have found wide clinical applications (Wakeling et al, 1996;Grünwald and Hidalgo, 2003;Wakeling, 2005;Wedge et al, 2005;Liu et al, 2007;Lüth and Löwe, 2008;Li et al, 2010). In a recent approach, the antitumor activity of quinazoline derivatives has shown to be enhanced by introducing sulfonamide-containing moieties substituted at position 4, as revealed in compounds III and IV which are potent inhibitors of EGFR PTK (Abouzid and Shouman, 2008) (Fig.…”

Synthesis, Characterisation and Biological Evaluation of Quinazoline Derivatives as Novel Anti-Microbial Agents

“…In the present work, the starting quinazoline-2,4-diol (2) was prepared from 2-aminobenzoic acid (1) and Urea according to synthetic procedure was prepared according to synthetic procedure [37]. 2,4-dichloroquinazoline (3) was prepared according to synthetic procedure [38].…”

Microwave-Assisted Synthesis of Bioactive Six-Membered Heterocycles and Their Fused Analogues

“…Doxazosin mesylate (187, Cardura ® ), a drug used in the treatment of hypertension [184], gefitinib (188, Iressa ® ) and erlotinib (189, Tarceva ® ) are epidermal growth factor receptor inhibitors approved for the treatment of lung cancer and are relevant examples of marketed drugs encompassing such heterocyclic motive [185,186] (Figure 13). The newly synthesized pyridopyrimidine derivatives were evaluated in vitro for their potencies as inhibitors of the acetyl-cholinesterase (AChE) and the butyrylcholinesterase (BChE).…”

“…Doxazosin mesylate (187, Cardura ® ), a drug used in the treatment of hypertension [184], gefitinib (188, Iressa ® ) and erlotinib (189, Tarceva ® ) are epidermal growth factor receptor inhibitors approved for the treatment of lung cancer and are relevant examples of marketed drugs encompassing such heterocyclic motive [185,186] (Figure 13). In the last decade, numerous syntheses of highly functionalized series of quinazoline derivatives have been described in the literature [187][188][189][190][191][192][193][194][195][196][197][198][199].…”