| 摘要 |
PURPOSE: Provided are novel adenine compounds which inhibit the cyclin dependent kinase (CDK), specifically, isopropylpurine derivatives with the substitution at C-2,6,9 positions and their preparation method. These adenine compounds are more effective than existing olomousine and roscovitine in CDK inhibition. CONSTITUTION: The compounds are represented by chemical formula 1, wherein R1 is piperidino, piperazino, pyrrolidino or thiomorpholino group which is substituted by one or more groups selected from hydroxyalkyl amino, hydroxy, hydroxyalkyl, carboxylic acid, aldehyde and oxim group. Most preferably R1 is hydroxyalkylamino or 4-carboxy-2-hydroxymethyl pyrrolidino group. The preparation process includes the steps of: reacting 2,6-dichloropurine with 3-chloroaniline in butanol solution; reacting the resultant compound with isopropyl halide in the presence of strong base and reacting the product, in 4:1 mixed solvent of n-butanol and DMSO, with piperidine, piperazino, pyrrolidino or thiomorpholino group which is substituted by one or more group selected from hydroxyalkyl amino, hydroxy, hydroxyalkyl, carboxylic acid, aldehyde and oxim group.
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