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Volumn 20, Issue 20, 2010, Pages 5984-5987

Pyrazolobenzodiazepines: Part I. Synthesis and SAR of a potent class of kinase inhibitors

Author keywords

Antitumor agents; CDK2; Kinase inhibitors; Pyrazolobenzodiazepines

Indexed keywords

2,1,3 BENZOTHIADIAZOLE; DYE; TIZANIDINE; UNCLASSIFIED DRUG;

EID: 77956913972     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.08.079     Document Type: Article
Times cited : (13)

References (22)
  • 1
    • 67650073265 scopus 로고    scopus 로고
    • While the initial rationale for developing a CDK2 selective inhibitor inspired the undertaking of this work, the continuing examination of the cell cycle has revealed that the roles of the CDKs are more complex. Reviews on the more recent aspects may be found in: S. Lapenna, and A. Giordano Nat. Rev. Drug Disc. 8 2009 547
    • (2009) Nat. Rev. Drug Disc. , vol.8 , pp. 547
    • Lapenna, S.1    Giordano, A.2
  • 16
    • 77956926985 scopus 로고    scopus 로고
    • note
    • Crystals of the CDK2:3a complex were grown at 4 °C by the vapor diffusion method. CDK2(1-298) at 12 mg/mL was mixed with a five molar excess of compound and equilibrated against 10% PEG 3350, 0.2 M ammonium fluoride, 0.1 M Tris pH 8.5. 0.2% DTT was added to the reservoir after mixing of the drop. Cryoprotectant was the same as the reservoir with 20% PEG 3350 and the addition of 15% ethylene glycol. X-ray data was collected at beamline X8C at Brookhaven National Laboratories. Data was processed to 2.0 with the HKL package (Otwinowski, Z., Minor, W. Methods Enzymol. 1997, 276, 307). The structure was determined by molecular replacement using AmoRe (Navaza, J. Acta Crystallogr. 1994, A50, 157) and was refined with CNX (CNX v.99.0-BETA, Molecular Simulations Inc.) to an R-factor/Rfree of 0.196/0.243. The structure has been deposited to the PDB with the code 3LE6.
  • 19
    • 0030952289 scopus 로고    scopus 로고
    • W. Risau Nature 386 1997 671
    • (1997) Nature , vol.386 , pp. 671
    • Risau, W.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.