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Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors.

Bioorganic & medicinal chemistry letters 2004 Aug 2; 14(15):3925-8

Link to PubMed abstract

Al-awar R RS, Ray J JE, Hecker K KA, Joseph S S, Huang J J, Shih C C, Brooks H HB, Spencer C CD, Watkins S SA, Schultz R RM, Considine E EL, Faul M MM, Sullivan K KA, Kolis S SP, Carr M MA, Zhang F F

Discovery Chemistry Research, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA. al-awar_rima_s@lilly.com

The synthesis of novel aza-1,7-annulated indoles was achieved and these were converted to indolocarbazoles that proved to be potent kinase inhibitors. These compounds were also evaluated in a human colon carcinoma cell line and proved to be good antiproliferative agents.