☆ 4.7 Article

Pyrazolo[1,5-a]-1,3,5-triazine as a Purine Bioisostere: Access to Potent Cyclin-Dependent Kinase Inhibitor (R)-Roscovitine Analogue

JOURNAL OF MEDICINAL CHEMISTRY (2009)

期刊

JOURNAL OF MEDICINAL CHEMISTRY

卷 52, 期 3, 页码 655-663

出版社

AMER CHEMICAL SOC

DOI: 10.1021/jm801340z

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Chemistry, Medicinal

资金

EEC
Canceropole Grand-Ouest
Institut National du Cancer (INCa)
Cancer Detection d'Innovations 2006
Ligue Nationale contre le Cancer
U.S. NIH [PO1-CA74175]
Ministere de la Recherche
Association pour la Recherche sur le Cancer

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Pharmacological inhibitors of cyclin-dependent kinases (CDKs) have a wide therapeutic potential. Among the CDK inhibitors currently under clinical trials, the 2,6,9-trisubstituted purine (R)-roscovitine displays rather high selectivity, low toxicity, and promising antitumor activity. In an effort to improve this structure, we synthesized several bioisosteres of roscovitine. Surprisingly, one of them, pyrazolo[1,5-a]-1,3,5-triazine 7a (N-&-N1, GP0210), displayed significantly higher potency, compared to (R)-roscovitine and imidazo[2,1-f]-1,2,4-triazine 13 (N-&-N2, GP0212), at inhibiting various CDKs and at inducing cell death in a wide variety of human tumor cell lines. This approach may thus provide second generation analogues with enhanced biomedical potential.

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