Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 7, 1998, Pages 793-798

  Legraverend, Michel ^a   Ludwig, Odile ^a   Bisagni, Emile ^a   Leclerc, Sophie ^b   Meijer, Laurent ^b  

^a CNRS   (France)

^b STATION BIOLOGIQUE   (France)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLIN B; CYCLIN DEPENDENT KINASE; CYCLIN DEPENDENT KINASE INHIBITOR; OLOMOUCINE; PURINE DERIVATIVE; ROSCOVITINE; UNCLASSIFIED DRUG;

ARTICLE; CELL CYCLE; DRUG SYNTHESIS; HYDROGENATION; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION;

ALKYNES; ANIMALS; CDC2 PROTEIN KINASE; CYCLIN B; CYCLIN-DEPENDENT KINASES; ENZYME INHIBITORS; FEMALE; KINETIN; OOCYTES; PURINES; STARFISH; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0032492705     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00097-3     Document Type: Article

References (18)

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14. 50's were calculated from inhibitor dose-response curves.
15. 12. Physical data for compounds 2a-h, 3a-f and 4 are as shown below: (table presented)
16. 3 at 200 MHz are shown below:
17. 2CH, J=6.7).
18. 14. Modifications at the N9 position have been explored in our laboratory. So far an isopropyl residue provides the most active derivatives (unpublished results). We have not yet explored the effects of modifications of the N6 substituent which have been claimed recently to enhance the inhibitory activity of Olomoucine. (Norman, T. C.; Gray, N. S.; Koh, J. T.; Schultz, P. G. J. Am. Chem. Soc. 1996, 118, 7430-7431.