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A Stepwise Approach for the Synthesis of Folic Acid Conjugates with Protein Kinase Inhibitors
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SYSNO ASEP 0485773 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title A Stepwise Approach for the Synthesis of Folic Acid Conjugates with Protein Kinase Inhibitors Author(s) Krajčovičová, S. (CZ)
Gucký, Tomáš (UEB-Q) ORCID
Hendrychová, Denisa (UEB-Q) ORCID
Kryštof, Vladimír (UEB-Q) RID, ORCID
Soural, M. (CZ)Number of authors 5 Source Title Journal of Organic Chemistry. - : American Chemical Society - ISSN 0022-3263
Roč. 82, č. 24 (2017), s. 13530-13541Number of pages 12 s. Language eng - English Country US - United States Keywords CYCLIN-DEPENDENT KINASES ; FOLATE RECEPTOR ; REGIOSELECTIVE SYNTHESIS Subject RIV FR - Pharmacology ; Medidal Chemistry OECD category Organic chemistry R&D Projects GA15-15264S GA ČR - Czech Science Foundation (CSF) LO1304 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) Institutional support UEB-Q - RVO:61389030 UT WOS 000418392600056 EID SCOPUS 85037594836 DOI 10.1021/acs.joc.7b02650 Annotation 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. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2018
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