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Volumn 17, Issue 23, 2007, Pages 6567-6571

Hit generation and exploration: Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases

Author keywords

Aurora; Imidazo 4,5 b pyridines; Kinases

Indexed keywords

(2 (4 (6 CHLORO 2 (4 DIMETHYLAMINO)PHENYL) 3H IMIDAZO[4,5 B]PYRIDIN 7 YL)PIPERAZIN 1 YL) N (THIZOL 2 YL)ACETAMIDE; AURORA KINASE INHIBITOR; IMIDAZO[4,5 B]PYRIDINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 35649014837     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.09.076     Document Type: Article
Times cited : (89)

References (29)
  • 18
    • 0033801916 scopus 로고    scopus 로고
    • For synthetic approaches to benzimidazoles and imidazopyridines also see
    • For synthetic approaches to benzimidazoles and imidazopyridines also see. Singh M.P., Sasmal S., Lu W., and Chatterjee M.N. Synthesis (2000) 1380
    • (2000) Synthesis , pp. 1380
    • Singh, M.P.1    Sasmal, S.2    Lu, W.3    Chatterjee, M.N.4
  • 19
    • 35648996395 scopus 로고    scopus 로고
    • Bavetsias, V.; McDonald, E.; Linardopoulos, S. Patent WO 2007/072017 A2, 2007.
  • 21
    • 35648978897 scopus 로고    scopus 로고
    • note
    • For clarity, imidazo[4,5-b]pyridines are represented in a single tautomeric form.
  • 25
    • 35648989934 scopus 로고    scopus 로고
    • 2,3-Diamino-4,5-dichloropyridine, required for the synthesis of 27, was prepared by reducing 2-amino-4,5-dichloro-3-nitropyridine as described in: Johanson, H.; Lawitz, K.; Nikitidis, G.; Sjo, P.; Storm, P. Patent WO 2004016611 A1. Likewise, 4-chloro-2,3-diaminopyridine, required for the synthesis of 29, was prepared from 2-amino-4-chloro-3-nitropyridine by applying the same methodology.
  • 26
    • 35649028630 scopus 로고    scopus 로고
    • note
    • 50 values were determined using either the Flashplate assay as described in Ref. 14, or the Filterplate assay as described in Ref. 17. ATP concentration in the assay is 20 μM.
  • 27
    • 35649013693 scopus 로고    scopus 로고
    • note
    • 3).
  • 28
    • 35649020661 scopus 로고    scopus 로고
    • note
    • Inhibition of human liver CYP isozymes was assessed in human liver microsomes (pool of 50 individuals) as described in Ref. 27 with the following modifications: microsomal protein concentration 0.5 mg/ml, incubation time 10 min, mephenytoin as the CYP2C19 substrate and metabolite detection by LC-MS-MS ESI+ on a Shimadzu LC system connected to a QTRAP 4000 (Applied Biosystems).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.