| 12392733 |
Krystof V, Lenobel R, Havlicek L, Kuzma M, Strnad M: Synthesis and biological activity of olomoucine II. Bioorg Med Chem Lett. 2002 Nov 18;12(22):3283-6.
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-isopropylp urine, 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. |
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