Casein kinase II (CK2) is an intensively studied enzyme, involved in different\ndiseases, cancer in particular. Different scaffolds were used to develop inhibitors of this\nenzyme. Here, we report on the synthesis and biological evaluation of twenty phenolic,\nketonic, and para-quinonic indeno[1,2-b]indole derivatives as CK2 inhibitors. The most\nactive compounds were 5-isopropyl-1-methyl-5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-dione 4h\nand 1,3-dibromo-5-isopropyl-5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-dione 4w with identical\nIC50 values of 0.11 microM. Furthermore, the development of a QSAR model based on\nthe structure of indeno[1,2-b]indoles was performed. This model was used to predict\nthe activity of 25 compounds with naphtho[2,3-b]furan-4,9-dione derivatives, which were\npreviously predicted as CK2 inhibitors via a molecular modeling approach. The activities\nof four naphtho[2,3-b]furan-4,9-dione derivatives were determined in vitro and one of them\n(N-isopentyl-2-methyl-4,9-dioxo-4,9-dihydronaphtho[2,3-b]furan-3-carboxamide) turned out to inhibit\nCK2 with an IC50 value of 2.33 microM. All four candidates were able to reduce the cell viability by more\nthan 60% after 24 h of incubation using 10 microM.kinase II (CK2) is an intensively studied enzyme, involved in different\ndiseases, cancer in particular. Different scaffolds were used to develop inhibitors of this\nenzyme. Here, we report on the synthesis and biological evaluation of twenty phenolic,\nketonic, and para-quinonic indeno[1,2-b]indole derivatives as CK2 inhibitors. The most\nactive compounds were 5-isopropyl-1-methyl-5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-dione 4h\nand 1,3-dibromo-5-isopropyl-5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-dione 4w with identical\nIC50 values of 0.11 microM. Furthermore, the development of a QSAR model based on\nthe structure of indeno[1,2-b]indoles was performed. This model was used to predict\nthe activity of 25 compounds with naphtho[2,3-b]furan-4,9-dione derivatives, which were\npreviously predicted as CK2 inhibitors via a molecular modeling approach. The activities\nof four naphtho[2,3-b]furan-4,9-dione derivatives were determined in vitro and one of them\n(N-isopentyl-2-methyl-4,9-dioxo-4,9-dihydronaphtho[2,3-b]furan-3-carboxamide) turned out to inhibit\nCK2 with an IC50 value of 2.33 microM. All four candidates were able to reduce the cell viability by more\nthan 60% after 24 h of incubation using 10 microM.
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