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Novel bis-(1H-indol-2-yl)-methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase

Mahboobi, Siavosh and Uecker, A. and Sellmer, A. and Cénac, C. and Höcher, H. and Pongratz, H. and Hufsky, H. and Trümpler, A. and Sicker, M. and Heidel, F. and Fischer, T. and Stocking, C. and Elz, Sigurd and Böhmer, F.-D. and Dove, Stefan (2006) Novel bis-(1H-indol-2-yl)-methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. Journal of Medicinal Chemistry 49 (11), pp. 3101-3115.

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Other URL: http://pubs.acs.org/doi/abs/10.1021/jm058033i


Abstract

FLT3 receptor tyrosine kinase is aberrantly active in many cases of acute myeloid leukemia (AML). Recently, bis(1H-indol-2-yl)methanones were found to inhibit FLT3 and PDGFR kinases. To optimize FLT3 activity and selectivity, 35 novel derivs. were synthesized and tested for inhibition of FLT3 and PDGFR autophosphorylation. The most potent FLT3 inhibitors I and II show IC50 values of 0.06 and ...

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Item Type:Article
Date:2006
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)
Projects:Deutsche Krebshilfe 10-2100
Identification Number:
ValueType
2006:429474Other
Subjects:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
600 Technology > 610 Medical sciences Medicine
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Partially
Owner: Prof. Dr. Stefan Dove
Deposited On:20 Jan 2009 16:45
Last Modified:05 Aug 2009 13:50
Item ID:5450
Owner Only: item control page
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