7-azaindole is well known as a kinase privileged fragment[1-2] and has been incorporated into many kinase inhibitors as a hinge-binding element[3]. It has multiple modification sites where various substituents can be readily attached. Therefore recent years have seen growing interest in this 7-azaindole scaffold and more than 100000 chemical structures having 7-azaindole framework have been registered in the CAS chemical database, which is steadily increasing by the synthetic innovation and enrichment of commercially available derivatives[3]. Most importantly, 7-azaindole fragment have been used as a starting point of medicinal chemistry targeting various kinases[3]. According to statistics, many drug molecules containing 7-azindole have been marketed or are currently under clinical study[3-8]..
[1] Journal of Medicinal Chemistry (2008), 51(17), 5149-5171.
[2] Bioorganic & Medicinal Chemistry Letters (2008), 18(16), 4610-4614.
[3] Chemical & Pharmaceutical Bulletin (2018), 66(1), 29-36.
[4] ACS Medicinal Chemistry Letters (2020), 11(10), 1848-1854.
[5] Bioorganic Chemistry (2020), 94, 103474.
[6] European Journal of Medicinal Chemistry (2018), 145, 315-327.
[7] Nature Reviews Drug Discovery (2012), 11(11), 873-886.
[8] Nature (2015), 526(7574), 583-586.
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