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Inhibition of PDGFR tyrosine kinase activity by a series of novel N-(3-(4-(pyridin-3-yl)-1H-imidazol-2-ylamino)phenyl)amides: a SAR study on the bioisosterism of pyrimidine and imidazole

Mahboobi, Siavosh and Sellmer, Andreas and Eswayah, Asma and Elz, Sigurd and Uecker, Andrea and Böhmer, Frank-D. (2008) Inhibition of PDGFR tyrosine kinase activity by a series of novel N-(3-(4-(pyridin-3-yl)-1H-imidazol-2-ylamino)phenyl)amides: a SAR study on the bioisosterism of pyrimidine and imidazole. European journal of medicinal chemistry 43 (7), pp. 1444-1453.

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Abstract

A series of N-(3-(4-(pyridin-3-yl)-1H-imidazol-2-ylamino)phenyl)amides were synthesized and tested for inhibition of PDGFR and FLT3 autophosphorylation. The novel N-(3-(4-(pyridin-3-yl)-1H-imidazol-2-ylamino)phenyl)amides, obtained by replacement of the pyrimidine system in Imatinib (1) with an imidazole ring, exhibit potent inhibitory activity on PDGFR, similar to the parent compound (IC(50) ...

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Item Type:Article
Date:2008
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)
Identification Number:
ValueType
17983688PubMed ID
10.1016/j.ejmech.2007.09.021DOI
Classification:
NotationType
Imidazoles/chemistryMESH
Magnetic Resonance SpectroscopyMESH
Pyrimidines/chemistryMESH
Receptors, Platelet-Derived Growth Factor/antagonists & inhibitorsMESH
Spectrometry, Mass, Electrospray IonizationMESH
Structure-Activity RelationshipMESH
Subjects:500 Science > 570 Life sciences
600 Technology > 610 Medical sciences Medicine
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Partially
Owner: Ute Lange
Deposited On:09 Feb 2009 11:25
Last Modified:05 Aug 2009 13:50
Item ID:5668
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