Mahboobi, Siavosh and Sellmer, Andreas and Eswayah, Asma and Elz, Sigurd and Uecker, Andrea and Boehmer, 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. ISSN 0223-5234,
Full text not available from this repository. (Request a copy)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) (9e) = 0.2 mu M; IC(50) Imatinib (1) = 0.3 mu M). Selectivity hereby seems to be conserved, as shown by the lack of activity on FLT3, a closely related class III receptor tyrosine kinase, which is not affected by the parent compound Imatinib. (c) 2007 Elsevier Masson SAS. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | RECEPTORS; IMATINIB; POTENT; DERIVATIVES; TARGETS; DRUG; PAP; 1H-imidazol-2-ylamine; pyrimidine; receptor tyrosine kinase; PDGFR; bioisosterism |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 28 Oct 2020 09:52 |
| Last Modified: | 28 Oct 2020 09:52 |
| URI: | https://pred.uni-regensburg.de/id/eprint/30655 |
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