메뉴 건너뛰기




Volumn 18, Issue 17, 2008, Pages 4844-4848

Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors

Author keywords

KDR inhibitor; Kinase inhibitor; VEGFR 2 inhibitor

Indexed keywords

INDAZOLE DERIVATIVE; VASCULOTROPIN; VASCULOTROPIN RECEPTOR 2;

EID: 49949083836     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.07.080     Document Type: Article
Times cited : (21)

References (20)
  • 7
    • 49949107642 scopus 로고    scopus 로고
    • Manuscript in preparation.
    • Manuscript in preparation.
  • 8
    • 49949088040 scopus 로고    scopus 로고
    • Potashman, M. H.; Kim, T.-S.; Bellon, S.; Booker, S.; Cheng, Y.; Kim, J. L.; Tasker, A.; Xi, N.; Xu, S.; Harmange, J.-C.; Borg, G.; Weiss, M.; Hodous, B. L.; Graceffa, R.; Buckner, W. H.; Masse, C. E.; Choquette, D.; Martin, M. W.; Germain, J.; Dipietro, L. V.; Chaffee, S. C.; Nunes, J. J.; Buchanan, J. L.; Habgood, G. J.; McGowan, D. C.; Whittington, D. A. PCT Int. Appl., WO 2005070891, 2005.
    • Potashman, M. H.; Kim, T.-S.; Bellon, S.; Booker, S.; Cheng, Y.; Kim, J. L.; Tasker, A.; Xi, N.; Xu, S.; Harmange, J.-C.; Borg, G.; Weiss, M.; Hodous, B. L.; Graceffa, R.; Buckner, W. H.; Masse, C. E.; Choquette, D.; Martin, M. W.; Germain, J.; Dipietro, L. V.; Chaffee, S. C.; Nunes, J. J.; Buchanan, J. L.; Habgood, G. J.; McGowan, D. C.; Whittington, D. A. PCT Int. Appl., WO 2005070891, 2005.
  • 13
    • 49949093190 scopus 로고    scopus 로고
    • note
    • c Log P values were calculated employing software from ACD Labs (Advanced Chemistry Development Inc.).
  • 15
    • 49949107842 scopus 로고    scopus 로고
    • note
    • No inhibition of tissue growth is desired as the target is the selective inhibition of angiogenesis. See Ref. 9 for further detail.
  • 16
    • 49949102761 scopus 로고    scopus 로고
    • note
    • 50 > 1 μM.
  • 17
    • 49949109386 scopus 로고    scopus 로고
    • note
    • See Supporting information.
  • 19
    • 49949090533 scopus 로고    scopus 로고
    • note
    • Male Sprague-Dawley rats were dosed via femoral vein (intravenous, DMSO solution, dose 1 mg/kg) or via oral gavage (suspensions in Ora-Plus, pH adjusted to a range of 2.0-2.2 using methanesulfonic acid, dose 10 mg/kg). Concentrations of all formulations were selected to allow for dose volumes in accordance with the highest scientific, humane, and ethical principles as defined by IACUC (Institutional Animal Care and Use Committees). Serial blood samples were collected from jugular vein into heparized tubes for over a 12-24 h period. Plasma was separated by centrifugation, and the sample was prepared for analysis by protein precipitation with acetonitrile. Quantitation of the test compounds was accomplished by reverse phase liquid chromatography with mass spectral detection in multiple reaction monitoring mode, with an appropriate internal standard. Pharmacokinetic parameters such as clearance, volume of distribution, and terminal half-life were calculated by a noncompartmental method.
  • 20
    • 84940142489 scopus 로고
    • 5 VEGF-expressing or vector control HEK 293 cells were mixed with Matrigel and injected subcutaneously on the ventral surface of nude mice. Approximately 24 h later, a single oral dose of compound or vehicle was administered. After 6 h, the mice received an intravenous injection of 0.1 mL 1% Evan's blue dye for 10 min prior to sacrifice.
    • 4. Data represent mean ± standard error; n = 5 per group. Statistical analysis was performed by one-way ANOVA with Bonferroni-Dunn post-hoc test. p < 0.0009 was considered significant
    • (1952) J. Physiol. , vol.118 , pp. 228
    • Miles, A.A.1    Miles, E.M.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.