메뉴 건너뛰기




Volumn 19, Issue 4, 2009, Pages 1240-1244

Development of thioquinazolinones, allosteric Chk1 kinase inhibitors

Author keywords

Allosteric kinase inhibitor; Chk1; Thioquinazolinone; X ray crystal structure

Indexed keywords

ADENOSINE TRIPHOSPHATE; CHECKPOINT KINASE 1; CHECKPOINT KINASE 1 INHIBITOR; PROTEIN SERINE THREONINE KINASE INHIBITOR; QUINAZOLINONE DERIVATIVE; THIOQUINAZOLINONE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 59649092904     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.12.076     Document Type: Article
Times cited : (82)

References (27)
  • 16
    • 59649099379 scopus 로고    scopus 로고
    • PCT Int. Appl. WO 2007015837
    • Fraley, M. E.; Steen, J. T. PCT Int. Appl. WO 2007015837, 2007.
    • (2007)
    • Fraley, M.E.1    Steen, J.T.2
  • 22
    • 59649112039 scopus 로고    scopus 로고
    • note
    • 3+ to XL665, and fluorescence emission from XL665 at 665 nm. In this assay, an inhibitor of Chk1 enzyme could be detected by a decrease of fluorescence.
  • 24
    • 59649128833 scopus 로고    scopus 로고
    • note
    • 3CN gradient w/0.1% TFA present) to yield pure product 5.
  • 25
    • 19944433628 scopus 로고    scopus 로고
    • note
    • 50 values.
  • 26
    • 59649125145 scopus 로고    scopus 로고
    • note
    • sym = 0.066 and completeness = 98%, respectively. The complex structures were refined to an R-factor of 0.182. The chlorobenzene ring of compound 38 has two conformations at 70% and 30% occupancies, respectively. The detailed X-ray diffraction data and refinement statistics are listed under PDB code 3F9N at the protein data bank. The crystallographic parameters are reported in the supporting information for this article.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.