Development of novel benzotriazines for drug discovery.

Abstract

BACKGROUND:

The synthesis of novel benzotriazine heterocycles was developed independently around the same time by Bischler, Bamberger and Arndt. Over the years, different groups have reported the synthesis of benzotriazine based compounds.

OBJECTIVE:

This literature review gives an update on recent benzotriazine compounds and their applications.

CONCLUSION:

The benzotriazine core has been used in various drug discovery projects including anticancer, anti-inflammatory and antimalarial programs. Recently, the benzotriazine core was used to develop selective kinase inhibitors targeting SRC, VEGFr2, BCR-ABL and BCR-ABL-T315I. Two benzotriazine based compounds, tirapazamine for the treatment of cancer and TG100801 for the treatment of age-related macular degeneration, have entered clinical trials.

• Authors: Moorthy Ss Palanki, Jianguo Cao, Chun P Chow, Elena Dneprovskaia, Chi Ching Mak, Andrew McPherson, Ved P Pathak, Joel Renick, Richard Soll, Binqi Zeng, Glenn Noronha
• Journal: Expert opinion on drug discovery (Expert Opin Drug Discov) Vol. 4 Issue 1 Pg. 33-49 (Jan 2009) ISSN: 1746-0441 [Print] England
• PMID: 23480335 (Publication Type: Journal Article)