Issue 5, 2014

Novel inhibitors of breast cancer relevant kinases Brk and HER2

Abstract

Novel 4-anilino pyrido[2,3-b]indoles have been discovered as inhibitors of the breast cancer relevant protein kinase Brk. Within this first series favourable aniline substituents have been characterized. Combinations with substituents of the molecular scaffold have been further investigated and led to additional nanomolar Brk inhibitors. Due to the reported role of Brk in breast cancer progression via HER2 activation we determined the inhibition profile of our novel Brk inhibitors to additionally inhibit HER2. These studies characterized the first dually acting Brk and HER2 inhibitor and the first exclusive HER2 inhibitors.

Graphical abstract: Novel inhibitors of breast cancer relevant kinases Brk and HER2

Supplementary files

Article information

Article type
Concise Article
Submitted
22 Jan 2014
Accepted
06 Feb 2014
First published
31 Mar 2014

Med. Chem. Commun., 2014,5, 659-664

Novel inhibitors of breast cancer relevant kinases Brk and HER2

K. A. Mahmoud, T. Wersig, I. Slynko, F. Totzke, C. Schächtele, M. Oelze, W. Sippl, C. Ritter and A. Hilgeroth, Med. Chem. Commun., 2014, 5, 659 DOI: 10.1039/C4MD00028E

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Spotlight

Advertisements