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Pyrazolo[4,3-d]pyrimidine Bioisostere of Roscovitine: Evaluation of a Novel Selective Inhibitor of Cyclin-Dependent Kinases with Antiproliferative Activity
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SYSNO ASEP 0368592 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Pyrazolo[4,3-d]pyrimidine Bioisostere of Roscovitine: Evaluation of a Novel Selective Inhibitor of Cyclin-Dependent Kinases with Antiproliferative Activity Author(s) Jorda, Radek (UEB-Q) ORCID, RID
Havlíček, Libor (UEB-Q) RID, ORCID
McNae, I. W. (GB)
Walkinshaw, M. D. (GB)
Voller, Jiří (UEB-Q) RID, ORCID
Šturc, Antonín (UEB-Q)
Navrátilová, Jana (UEB-Q)
Kuzma, Marek (MBU-M) ORCID, RID
Mistrik, M. (CZ)
Bártek, J. (CZ)
Strnad, Miroslav (UEB-Q) RID, ORCID
Kryštof, Vladimír (UEB-Q) RID, ORCIDNumber of authors 12 Source Title Journal of Medicinal Chemistry. - : American Chemical Society - ISSN 0022-2623
Roč. 54, č. 8 (2011), s. 2980-2993Number of pages 14 s. Language eng - English Country US - United States Keywords STRUCTURE-GUIDED DESIGN ; DNA-END RESECTION ; DOWN-REGULATION ; R-ROSCOVITINE ; CELL-CYCLE Subject RIV ED - Physiology R&D Projects GA301/02/0475 GA ČR - Czech Science Foundation (CSF) GA301/08/1649 GA ČR - Czech Science Foundation (CSF) ED0007/01/01 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) CEZ AV0Z50380511 - UEB-Q (2005-2011) AV0Z50200510 - MBU-M (2005-2011) UT WOS 000289697800033 DOI 10.1021/jm200064p Annotation Inhibition of cyclin-dependent kinases (CDKs) with. small molecules has been suggested as a strategy for treatment of cancer, based on deregulation of CDKs commonly found in many types of human tumors. Here, a new potent CDK2 inhibitor with pyrazolo[4,3-d]pyrimidine scaffold has been synthesized, characterized, and evaluated in cellular and biochemical assays. 7-Benzylamino-5(R)-[2-(hydroxymethyl)-propyl]amino-3-isopropyl-1(2)H-pyrazolo[4,3-d]pyrimidine, compound 7, was prepared as a bioisostere of the well-known CDK inhibitor roscovitine. An X-ray crystal structure of compound 7 bound to CDK2 has been determined, revealing a binding mode similar to that of roscovitine. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2012
Number of the records: 1