0172263 - UEB-Q 20023048 RIV GB eng J - Journal Article
Kryštof, Vladimír - Lenobel, R. - Havlíček, Libor - Kuzma, Marek - Strnad, Miroslav
Synthesis and biological activity of olomoucine II.
Bioorganic and Medicinal Chemistry Letters. Roč. 12, č. 22 (2002), s. 3283-3286. ISSN 0960-894X. E-ISSN 1464-3405
R&D Projects: GA MŠMT OC 844.10; GA ČR GA301/02/0475
Institutional research plan: CEZ:AV0Z5038910
Keywords : purine * olomoucine II * purvalanol A
Subject RIV: CE - Biochemistry
Impact factor: 2.051, year: 2002

Based on our previous experiences with synthesis of purines, novel 2,6,9-trisubstituted purine derivatives were prepared and assayed for the ability to inhibit CDK1/cyclin B kinase. One of newly synthesized compounds designated as olomoucine II, 6-[(2-hydroxybenzyl)amino]-2-{[1-(hydroxymethyl)propyl]amino}-9-isopropylpurine, displays 10 times higher inhibitory activity than roscovitine, potent and specific CDK1 inhibitor. Olomoucine II in vitro cytotoxic activity exceeds purvalanol A, the most potent CDK inhibitor, as it kills the CEM cells with IC50 value of 3.0 micro M.
Permanent Link: http://hdl.handle.net/11104/0069302