Beckers, Thomas and Sellmer, Andreas and Eichhorn, Emerich and Pongratz, Herwig and Schaechtele, Christoph and Totzke, Frank and Kelter, Gerhard and Krumbach, Rebekka and Fiebig, Heinz-Herbert and Boehmer, Frank-D. and Mahboobi, Siavosh (2012) Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones. BIOORGANIC & MEDICINAL CHEMISTRY, 20 (1). pp. 125-136. ISSN 0968-0896,
Full text not available from this repository. (Request a copy)Abstract
Several members of the quinazoline class of known tyrosine kinase inhibitors are approved anticancer agents, often showing selectivity for receptors of the HER/ErbB-family. Combining structural elements of this class with the bisindolylmethanone-structure led to a series of novel compounds. These compounds inhibited EGFR in the nanomolar range. Moreover, inhibition of EGFR autophosphorylation in intact A431 cells was shown, with IC50 values ranging form 0.3-1 mu M for compound 42, and 0.1-0.3 mu M for 45. In a panel of 42 human tumor cell lines the sensitivity profile of the novel compounds was shown to be similar to that of the quinazoline class of tyrosine kinase inhibitors lapatinib and erlotinib (Tarceva (R)). (C) 2011 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | INTERNATIONAL REFERENCE-STANDARD; SQUAMOUS-CELL CARCINOMA; POTENT INHIBITORS; TYROSINE KINASE; LUNG-CANCER; LINES; EXPRESSION; PROVIDES; HEAD; EGFR; Tyrosine kinase inhibitor; Anticancer agents; Bisindolylmethanone; Quinazoline; Epidermal growth factor receptor (EGFR) |
| 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: | 26 May 2020 09:29 |
| Last Modified: | 26 May 2020 09:30 |
| URI: | https://pred.uni-regensburg.de/id/eprint/19600 |
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