gms | German Medical Science

27th German Cancer Congress Berlin 2006

German Cancer Society (Frankfurt/M.)

22. - 26.03.2006, Berlin

Syntheses of Substituted 4-(Indol-3-yl)quinazolines, a New Class of EGFR-Tyrosinkinase Inhibitors

Meeting Abstract

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  • corresponding author presenting/speaker Anja Lüth - Freie Universität Berlin, Institut für Pharmazie, Deutschland
  • Werner Löwe - Freie Universität Berlin, Institut für Pharmazie
  • Peter Luger - Freie Universität Berlin, Institut für Kristallographie
  • Manuela Weber - Freie Universität Berlin, Institut für Kristallographie

27. Deutscher Krebskongress. Berlin, 22.-26.03.2006. Düsseldorf, Köln: German Medical Science; 2006. DocPO449

The electronic version of this article is the complete one and can be found online at: http://www.egms.de/en/meetings/dkk2006/06dkk559.shtml

Published: March 20, 2006

© 2006 Lüth et al.
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Outline

Text

Earlier investigations with inhibitors of the epidermal growth factor receptor (EGFR) family of tyrosine kinases led to the highly active 4-anilinoquinazolines Gefitinib (1) (Iressa®; Astra Zeneca) and Erlotinib (2) (Tarceva®; Genentech/OSI Pharmaceuticals/Roche).

We present the syntheses of the compounds (3), (4) and (5) in which the 4-anilino-moiety is exchanged by a substituted indol-3-yl heterocycle. Compounds (3), (4) and (5) represents a more fundamental change in the pharmacophore and claim an excellent EGFR-tyrosine kinase inhibition activity.

A detailed discussion of the synthetic results will be presented together with NMR-spectral, x-ray and pharmacologicalresults.

Figure 1 [Fig. 1].