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:

Published: March 20, 2006

© 2006 Lüth et al.
This is an Open Access article distributed under the terms of the Creative Commons Attribution License ( You are free: to Share – to copy, distribute and transmit the work, provided the original author and source are credited.



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].