title: Synthesis and biological activity of olomoucine II.
abstract: 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 IC(50) value of 3.0 microM.
authors.affiliation: Laboratory of Growth Regulators, Palacký University and Institute of Experimental Botany, Slechtitelů 11, 783 71 Olomouc, Czech Republic.
authors.forename: Vladimír
authors.initials: V
authors.lastname: Krystof
authors.forename: René
authors.initials: R
authors.lastname: Lenobel
authors.forename: Libor
authors.initials: L
authors.lastname: Havlícek
authors.forename: Marek
authors.initials: M
authors.lastname: Kuzma
authors.forename: Miroslav
authors.initials: M
authors.lastname: Strnad
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D016203:CDC2 Protein Kinase / Q000037:antagonists & inhibitors; D017489:CDC28 Protein Kinase, S cerevisiae / Q000037:antagonists & inhibitors; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D007701:Kinetin; D011687:Purines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000077546:Roscovitine; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: C471843:6-((3-chloro)anilino)-2-(isopropyl-2-hydroxyethylamino)-9-isopropylpurine; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011687:Purines; C475587:olomoucine II; D000077546:Roscovitine; C090046:olomoucine; D016203:CDC2 Protein Kinase; D017489:CDC28 Protein Kinase, S cerevisiae; D007701:Kinetin