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Volumn 18, Issue 21, 2008, Pages 5758-5762

Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors

Author keywords

Cancer; CDK2; CDK4; Cyclin dependant kinase inhibitor; GSK3 ; Pyrazolo 1,5 b pyridazine; VEGFR 2

Indexed keywords

AMINE; CYCLIN DEPENDENT KINASE 4; CYCLIN DEPENDENT KINASE INHIBITOR; GLYCOGEN SYNTHASE KINASE 3BETA; PYRAZOLE DERIVATIVE; PYRIDAZINE DERIVATIVE; VASCULOTROPIN RECEPTOR 2;

EID: 53949085747     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.09.069     Document Type: Article
Times cited : (33)

References (26)
  • 11
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    • Pyrazolo[1,5-b]pyridazines have been used as 5HT3-antagonists, Cox 2 inhibitors, and GSK-3β inhibitors
    • Pyrazolo[1,5-b]pyridazines have been used as 5HT3-antagonists, Cox 2 inhibitors, and GSK-3β inhibitors. Bondo H.J., Weis J., Suzdak P.D., and Eskesen K. Bioorg. Med. Chem. Lett. 45 (1994) 695
    • (1994) Bioorg. Med. Chem. Lett. , vol.45 , pp. 695
    • Bondo, H.J.1    Weis, J.2    Suzdak, P.D.3    Eskesen, K.4
  • 14
    • 53949110978 scopus 로고    scopus 로고
    • For full experimental details and spectral data on the preparation of pyrazolopyridazines, please see:
    • For full experimental details and spectral data on the preparation of pyrazolopyridazines, please see:. Harris P., Jung D., Peel M., Reno M., Rheault T., Stanford J., Stevens K., and Veal J. PCT Int. Appl. 134 (2003) WO 0351886
    • (2003) PCT Int. Appl. , vol.134
    • Harris, P.1    Jung, D.2    Peel, M.3    Reno, M.4    Rheault, T.5    Stanford, J.6    Stevens, K.7    Veal, J.8
  • 15
    • 0029029617 scopus 로고
    • The expression, purification and crystallization of CDK-2/Cyclin A was carried out as previously described Crystals were soaked with 50 μM compound for 2 days prior to data collections. The structures were refined to an Rfactor of 21% at 3.0 Å. The PDB deposition codes for the structures are 3EID and XXXX
    • The expression, purification and crystallization of CDK-2/Cyclin A was carried out as previously described. Jeffrey P.D., Russo A.A., Polyak K., Gibbs E., Hurwitz J., Massagué J., and Pavletich N.P. Nature 376 (1995) 313 Crystals were soaked with 50 μM compound for 2 days prior to data collections. The structures were refined to an Rfactor of 21% at 3.0 Å. The PDB deposition codes for the structures are 3EID and XXXX
    • (1995) Nature , vol.376 , pp. 313
    • Jeffrey, P.D.1    Russo, A.A.2    Polyak, K.3    Gibbs, E.4    Hurwitz, J.5    Massagué, J.6    Pavletich, N.P.7
  • 16
    • 53949091632 scopus 로고    scopus 로고
    • Image generated with PyMol (Delano Scientific).
    • Image generated with PyMol (Delano Scientific).
  • 22
    • 53949107887 scopus 로고    scopus 로고
    • note
    • 2, 0.3 mg/mL heparin, 0.1 mg/mL BSA, 1 mM DTT, 2.5 μM ATP, 0.0066 Ci/uL 33P-ATP, and 1.2 μg/mL GSK3β protein were prepared in polystyrene plates. The reactions were started by addition of enzyme to substrate and were terminated by addition of 20 μL of stop solution [0.25 M EDTA, pH 8, 2.5 mM unlabelled ATP]. 195 μL of 1.3 mg/mL StreptAvidin-coated SPA beads in PBS were added and the plates counted in a Packard TopCount (1 min/well) after 10 h.
  • 23
    • 0037418786 scopus 로고    scopus 로고
    • Although we elucidated the demethylation conditions independently, there are examples of using morpholine for demethylations
    • Although we elucidated the demethylation conditions independently, there are examples of using morpholine for demethylations. Goclik V., and Mischnick P. Carbohydr. Res. 338 (2003) 733
    • (2003) Carbohydr. Res. , vol.338 , pp. 733
    • Goclik, V.1    Mischnick, P.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.