1135205-07-0Relevant academic research and scientific papers
Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors
Hundsd?rfer, Claas,Hemmerling, Hans-J?rg,G?tz, Claudia,Totzke, Frank,Bednarski, Patrick,Le Borgne, Marc,Jose, Joachim
, p. 2282 - 2289 (2012/05/07)
Herein we describe the synthesis and properties of indeno[1,2-b]indole derivatives as a novel class of potent inhibitors of the human protein kinase CK2. A set of 19 compounds was obtained using a convenient and straightforward synthesis protocol. The compounds were tested for inhibition of human protein kinase CK2, which was recombinantly expressed in Escherichia coli. New inhibitors with IC50 in the micro- and sub-micromolar range were identified. Compound 4b (5-isopropyl-7,8-dihydroindeno[1,2-b]indole-9,10(5H,6H)- dione) inhibited human CK2 with an IC50 of 0.11 μM and did not significantly inhibit 22 other human protein kinases, suggesting selectivity towards CK2. ATP-competitive inhibition by compound 4b was shown and a K i of 0.06 μM was determined. Our findings indicate that indeno[1,2-b]indoles are a promising starting point for further development and optimization of human protein kinase CK2 inhibitors.
