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Volumn 17, Issue 13, 2007, Pages 3618-3623

1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: Extended exploration on phenyl ring substitutions and preliminary ADME/PK studies

Author keywords

1,4 Dihydroindeno 1,2 c pyrazoles; Checkpoint kinase 1 inhibitors; Chk 1 inhibitors; Sensitizing DNA damaging agents

Indexed keywords

CHECKPOINT KINASE 1; DOXORUBICIN; PYRAZOLE DERIVATIVE;

EID: 34250196523     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.04.055     Document Type: Article
Times cited : (13)

References (18)
  • 9
    • 34250175370 scopus 로고    scopus 로고
    • Doyle, K.; Rafferty, P.; Steele, R.; Turner, A.; Wilkins, D.; Arnold, L. Therapeutic agents. US 6297238.
  • 12
    • 34250168909 scopus 로고    scopus 로고
    • note
    • Compounds 8 and 9 were synthesized from known starting materials, 5-hydroxy-2,3-dihydro-1H-inden-1-one and 3-iodo-1,4-dihydroindeno[1,2-c]pyrazole-6-carbaldehyde, respectively, following similar procedures shown in this article.
  • 13
    • 34250171070 scopus 로고    scopus 로고
    • note
    • 33P were used. The concentration of the vehicle, DMSO, in the final reaction is 2%. After 30 min at room temperature, the reaction was stopped by the addition of equal volume of 4 M NaCl and 0.1 M EDTA (pH 8.0). A 40 μL aliquot of the reaction mixture was added to a well in a Flash Plate (NEN Life Science Products, Boston, MA) containing 160 μL of phosphate-buffered saline (PBS) without calcium chloride and magnesium chloride and incubated at room temperature for 10 min. The plate was then washed three times in PBS with 0.05% of Tween 20 and counted in a Packard TopCount counter (Packard BioScience Company, Meriden, CT).
  • 14
    • 34250183687 scopus 로고    scopus 로고
    • note
    • See Ref. 4 for detailed X-ray co-crystal structures with coordinated deposited in the PDB.
  • 15
    • 34250181187 scopus 로고    scopus 로고
    • note
    • See Ref. 4 for assay conditions and representative raw data.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.