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Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones

Mahboobi, Siavosh and Uecker, A. and Cénac, C. and Sellmer, A. and Eichhorn, E. and Elz, Sigurd and Böhmer, F.-D. and Dove, Stefan (2007) Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones. Bioorganic & medicinal chemistry 15 (5), pp. 2187-2197.

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Other URL: http://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B6TF8-4MJJH05-4&_user=616165&_coverDate=03%2F01%2F2007&_rdoc=1&_fmt=&_orig=search&_sort=d&view=c&_acct=C000032338&_version=1&_urlVersion=0&_userid=616165&md5=5f36dd9dbdc950fa1555298c1f674434


A series of bis(benzo[b]furan-2-yl)methanones was synthesized and tested for inhibition of FLT3 and PDGFR autophosphorylation. Mostly, C-5 substitution leads to PDGFR selectivity, which was strongest in the case of the 5,5'-dimethoxy deriv. The 5,5'-diamino and the 6,6'-dihydroxy compds. are more active at FLT3. At both kinases, the potency of the best inhibitors approaches IC50 values of ...


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Item type:Article
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
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Dewey Decimal Classification:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
600 Technology > 610 Medical sciences Medicine
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Partially
Deposited on:20 Jan 2009 16:38
Last modified:05 Aug 2009 13:50
Item ID:5449
Owner only: item control page
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