A Stepwise Approach for the Synthesis of Folic Acid Conjugates with Protein Kinase Inhibitors
Jazyk angličtina Země Spojené státy americké Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
29171753
DOI
10.1021/acs.joc.7b02650
Knihovny.cz E-zdroje
- MeSH
- fluorescenční barviva chemie MeSH
- folátový receptor 1 účinky léků MeSH
- inhibitory proteinkinas chemie farmakologie MeSH
- kyselina listová chemie MeSH
- molekulární struktura MeSH
- průtoková cytometrie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- fluorescenční barviva MeSH
- folátový receptor 1 MeSH
- inhibitory proteinkinas MeSH
- kyselina listová MeSH
Herein, we report an alternative synthetic approach for selected 2,6,9-trisubstituted purine CDK inhibitor conjugates with folic acid as a drug-delivery system targeting folate receptors. In contrast to the previously reported approaches, the desired conjugates were constructed stepwise using solid-phase synthesis starting from immobilized primary amines. The ability of the prepared conjugates to release the free drug was verified using dithiothreitol (DTT) and glutathione (GSH) as liberating agents. Finally, binding to the folate receptor (FOLR1) overexpressed in a cancer cell line was measured by flow cytometry using a fluorescent imaging probe.
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