A Stepwise Approach for the Synthesis of Folic Acid Conjugates with Protein Kinase Inhibitors

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389030%3A_____%2F17%3A00485773" target="_blank" >RIV/61389030:_____/17:00485773 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1021/acs.joc.7b02650" target="_blank" >http://dx.doi.org/10.1021/acs.joc.7b02650</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/acs.joc.7b02650" target="_blank" >10.1021/acs.joc.7b02650</a>

Result language
angličtina
Original language name
A Stepwise Approach for the Synthesis of Folic Acid Conjugates with Protein Kinase Inhibitors
Original language description
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.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10401 - Organic chemistry

Project
<a href="/en/project/GA15-15264S" target="_blank" >GA15-15264S: Targeted Transport of Purine Cyclin-dependent Kinase Inhibitors into Cancer Cells</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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