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Expert Opinion on Drug Discovery Volume 4, 2009 - Issue 1
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Development of novel benzotriazines for drug discovery

Moorthy SS Palanki TargeGen, Inc., 9380 Judicial Drive, CA 92121, San Diego, USA +1 858 678 0760; +1 858 678 0762; [email protected]
,
Jianguo Cao TargeGen, Inc., 9380 Judicial Drive, CA 92121, San Diego, USA +1 858 678 0760; +1 858 678 0762; [email protected]
,
Chun P Chow TargeGen, Inc., 9380 Judicial Drive, CA 92121, San Diego, USA +1 858 678 0760; +1 858 678 0762; [email protected]
,
Elena Dneprovskaia TargeGen, Inc., 9380 Judicial Drive, CA 92121, San Diego, USA +1 858 678 0760; +1 858 678 0762; [email protected]
,
Chi Ching Mak TargeGen, Inc., 9380 Judicial Drive, CA 92121, San Diego, USA +1 858 678 0760; +1 858 678 0762; [email protected]
,
Andrew McPherson TargeGen, Inc., 9380 Judicial Drive, CA 92121, San Diego, USA +1 858 678 0760; +1 858 678 0762; [email protected]
,
Ved P Pathak TargeGen, Inc., 9380 Judicial Drive, CA 92121, San Diego, USA +1 858 678 0760; +1 858 678 0762; [email protected]
,
Joel Renick TargeGen, Inc., 9380 Judicial Drive, CA 92121, San Diego, USA +1 858 678 0760; +1 858 678 0762; [email protected]
,
Richard Soll TargeGen, Inc., 9380 Judicial Drive, CA 92121, San Diego, USA +1 858 678 0760; +1 858 678 0762; [email protected]
,
Binqi Zeng TargeGen, Inc., 9380 Judicial Drive, CA 92121, San Diego, USA +1 858 678 0760; +1 858 678 0762; [email protected]
&
Glenn Noronha TargeGen, Inc., 9380 Judicial Drive, CA 92121, San Diego, USA +1 858 678 0760; +1 858 678 0762; [email protected]
 show all
Pages 33-49 | Published online: 10 Dec 2008
 
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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.

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