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QSAR Model of Indeno[1,2-b]indole Derivatives and Identification of N-isopentyl-2-methyl-4,9-dioxo-4,9-Dihydronaphtho[2,3-b]furan-3-carboxamide as a Potent CK2 Inhibitor

Archive ouverte | Haidar, Samer | CCSD

International audience. Casein kinase II (CK2) is an intensively studied enzyme, involved in different diseases, cancer in particular. Different scaffolds were used to develop inhibitors of this enzyme. Here, we rep...

Converting potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2

Archive ouverte | Jabor Gozzi, Gustavo | CCSD

International audience. A series of indeno[1,2-b]indole-9,10-dione derivatives were synthesized as human casein kinase II (CK2) inhibitors. The most potent inhibitors contained a N(5)-isopropyl substituent on the C-...

Biological evaluation of 4,5,7-trisubstituted Indeno[1,2-b]indoles reveals a potent inhibitor of protein kinase CK2 in tumor cells with diverse anti-cancer effects and preferential cytoplasmic localization

Archive ouverte | Birus, Robin | CCSD

International audience. The highly pleiotropic and constitutively active serine/threonine protein kinase CK2 is considered a keytarget in cancer. The indeno[1,2-b]indole scaffold was previously shown to provide deri...

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