Probing the Anticancer Action of Novel Ferrocene Analogues of MNK Inhibitors
AbstractTwo novel ferrocene-containing compounds based upon a known MNK1/2 kinase (MAPK-interacting kinase) inhibitor have been synthesized. The compounds were designed to use the unique shape of ferrocene to exploit a large hydrophobic pocket in MNK1/2 that is only partially occupied by the original compound. Screening of the ferrocene analogues showed that both exhibited potent anticancer effects in several breast cancer and AML (acute myeloid leukemia) cell lines, despite a loss of MNK potency. The most potent ferrocene-based compound 5 was further analysed in vitro in MDA-MB-231 (triple negative breast cancer cells). Dose–response curves of compound 5 for 2D assay and 3D assay generated IC50 values (half maximal inhibitory concentration) of 0.55 µM and 1.25 µM, respectively. View Full-Text
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Sansook, S.; Lineham, E.; Hassell-Hart, S.; Tizzard, G.J.; Coles, S.J.; Spencer, J.; Morley, S.J. Probing the Anticancer Action of Novel Ferrocene Analogues of MNK Inhibitors. Molecules 2018, 23, 2126.
Sansook S, Lineham E, Hassell-Hart S, Tizzard GJ, Coles SJ, Spencer J, Morley SJ. Probing the Anticancer Action of Novel Ferrocene Analogues of MNK Inhibitors. Molecules. 2018; 23(9):2126.Chicago/Turabian Style
Sansook, Supojjanee; Lineham, Ella; Hassell-Hart, Storm; Tizzard, Graham J.; Coles, Simon J.; Spencer, John; Morley, Simon J. 2018. "Probing the Anticancer Action of Novel Ferrocene Analogues of MNK Inhibitors." Molecules 23, no. 9: 2126.
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