Article
N-Phenyl-4-hydroxy-2-quinolone-3-carboxamides as selective inhibitors of mutant H1047R phosphoinositide-3-kinase (PI3Kα).
Bioorganic & medicinal chemistry - 15 Dec 2012
Sabbah Dima A, Simms Neka A, Wang Wang, Dong Yuxiang, Ezell Edward L, Brattain Michael G, Vennerstrom Jonathan L, Zhong Haizhen A
Abstract excerpt
This work describes our efforts to optimize the lead PI3Kα inhibitor N-benzyl 4-hydroxy-2-quinolone-3-carboxamide using structure-based design and molecular docking. We identified a series of N-phenyl 4-hydroxy-2-quinolone-3-carboxamides as selective inhibitors of mutant H1047R versus wild-type PI3Kα and we also showed that the cell growth inhibition by these compounds likely occurs by inhibiting the formation of...
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