| 摘要 |
Use of purine derivatives (I) or their salts, hydrates, esters or isomers for the preparation of medicament intended to treat diseases in which an imbalance between the cell division and apoptosis is involved, is claimed. Use of purine derivatives of formula (I) or their salts, hydrates, esters or isomers for the preparation of medicament intended to treat diseases in which an imbalance between the cell division and apoptosis is involved, is claimed. X : C or N; Y1 : CH 3or OH; and Z : H or CH 3. An independent claim is included for the purine derivatives (I), preferably e.g. (R)-2-[9-isopropyl-6-(4-pyridin-2-yl-benzylamino)-9H- purin-2-ylamino]-butan-1-ol, (S)-2-[9-isopropyl-6-(4-pyridin-2-yl-ben zylamino)-9H-purin-2-ylamino]-butan-1-ol, 2-{6-[(biphenyl-4-ylmethyl) -amino]-9-isopropyl-9H-purin-2-ylamino}-butan-1-ol, 2-[9-isopropyl-6-(4-pyridin-2-yl-benzylamino)-9H-purin-2-ylamino]-pro pane-1,3-diol and (S)-2-amino-3-methyl-butyric acid (S)-2-[9-isopropyl-6-(4-pyridin-2-yl-benzylamino)-9H-purin-2-ylamino] -butyl ester. [Image] - ACTIVITY : Nephrotropic; Cytostatic. - MECHANISM OF ACTION : Cyclin-dependent kinase (CDK) inhibitor. The ability of (I) to inhibit CDK2 was tested using human recombinant CDK2 expressed in insect cells. The result showed that the (R)-2-[9-isopropyl-6-(4-pyridin-2-y l-benzylamino)-9H-purin-2-ylamino]-butan-1-ol exhibited an IC 5 0value of 0.041 mu M. |
