1415359-75-9Relevant academic research and scientific papers
N-Phenyl-4-hydroxy-2-quinolone-3-carboxamides as selective inhibitors of mutant H1047R phosphoinositide-3-kinase (PI3Kα)
Sabbah, Dima A.,Simms, Neka A.,Wang, Wang,Dong, Yuxiang,Ezell, Edward L.,Brattain, Michael G.,Vennerstrom, Jonathan L.,Zhong, Haizhen A.
, p. 7175 - 7183 (2012)
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 pAKT and induction of apoptosis.
