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Bis(1H-2-indolyl)methanones as a novel class of inhibitors of the platelet-derived growth factor receptor kinase

Mahboobi, Siavosh and Teller, S. and Pongratz, H. and Hufsky, H. and Sellmer, A. and Botzki, Alexander and Uecker, A. and Beckers, T. and Baasner, S. and Schächtele, C. and Überall, F. and Kassack, M. U. and Dove, Stefan and Böhmer, F.-D. (2002) Bis(1H-2-indolyl)methanones as a novel class of inhibitors of the platelet-derived growth factor receptor kinase. Journal of Medicinal Chemistry 45 (5), pp. 1002-1018.

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Other URL: http://pubs.acs.org/doi/abs/10.1021/jm010988n


Abstract

The novel lead bis(1H-2-indolyl)methanone inhibits autophosphorylation of platelet-derived growth factor (PDGF) receptor tyrosine kinase in intact cells. Various substituents in the 5- or 6-position of one indole ring increase or preserve potency, whereas most modifications of the ring structures and of the methanone group as well as substitution at both indoles result in weak or no activity. ...

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Item Type:Article
Date:2002
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
2002:80889Other
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 16:41
Last Modified:05 Aug 2009 13:50
Item ID:5448
Owner Only: item control page
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