1600515-44-3

Upstream product

• 95-53-4 o-toluidine 
• 25208-32-6 4-chloro-9-H-pyrido[2,3-b]indole 
• 13174-93-1 1-(pyridin-2-yl)-1H-benzo[d][1,2,3]triazole 
• 244-76-8 α-carboline 
• 95-14-7 1,2,3-Benzotriazole 
• 109-04-6 2-bromo-pyridine 
• 26148-55-0 9H-pyrido[2,3-b]indole 1-oxide 

Relevant academic research and scientific papers

Discovery of 4-anilino α-carbolines as novel Brk inhibitors

Dysregulation of cell signalling processes caused by an enhanced activity of protein kinases mainly contributes to cancer progression. Protein kinase inhibitors have been established as promising drugs that inhibit such overactive protein kinases in cancer cells. The formation of metastases, which makes a therapy difficult, remains a great challenge for cancer treatment. Recently, breast tumor kinase (Brk) was discovered as novel and interesting target for a cancer therapy because Brk participates in both cell dysregulation and metastasis. We discovered 4-anilino substituted α-carboline compounds as a novel class of highly active Brk inhibitors. In the current work, structure-activity relationships are discussed including docking results obtained for 4-anilino α-carbolines. A first profiling of selective kinase inhibition and a proof of concept for the antiproliferative effects is demonstrated. These results qualify the compounds as a promising class of novel antitumor agents.

Novel inhibitors of breast cancer relevant kinases Brk and HER2

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. This journal is the Partner Organisations 2014.