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Probing the Anticancer Action of Novel Ferrocene Analogues of MNK Inhibitors.
- Source :
-
Molecules (Basel, Switzerland) [Molecules] 2018 Aug 23; Vol. 23 (9). Date of Electronic Publication: 2018 Aug 23. - Publication Year :
- 2018
-
Abstract
- Two 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). Doseā»response curves of compound 5 for 2D assay and 3D assay generated IC <subscript>50</subscript> values (half maximal inhibitory concentration) of 0.55 µM and 1.25 µM, respectively.<br />Competing Interests: No conflicts of interest.
- Subjects :
- Antineoplastic Agents chemistry
Cell Line, Tumor
Cell Movement drug effects
Humans
Intracellular Signaling Peptides and Proteins antagonists & inhibitors
Leukemia, Myeloid, Acute metabolism
Protein Kinase Inhibitors chemistry
Protein Kinase Inhibitors pharmacology
Protein Serine-Threonine Kinases antagonists & inhibitors
Tamoxifen chemistry
Tamoxifen pharmacology
Triple Negative Breast Neoplasms metabolism
Antineoplastic Agents pharmacology
Ferrous Compounds chemistry
Metallocenes chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1420-3049
- Volume :
- 23
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Molecules (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 30142961
- Full Text :
- https://doi.org/10.3390/molecules23092126