Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376807 | Bioorganic & Medicinal Chemistry Letters | 2008 | 6 Pages |
Abstract
Fused dihydroindazolopyrrolocarbazole oximes have been identified as low nanomolar, potent dual TIE-2 and VEGF-R2 receptor tyrosine kinase inhibitors with excellent cellular potency. Development of the structure–activity relationships (SAR) led to identification of compounds 35 and 40 as potent, selective dual TIE-2/VEGF-R2 inhibitors with favorable pharmacokinetic properties. Compound 35 was orally active in tumor models with no observed toxicity.
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Related Topics
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Authors
Reddeppareddy Dandu, Allison L. Zulli, Edward R. Bacon, Ted Underiner, Candy Robinson, Hong Chang, Sheila Miknyoczki, Jennifer Grobelny, Bruce A. Ruggeri, Shi Yang, Mark S. Albom, Thelma S. Angeles, Lisa D. Aimone, Robert L. Hudkins,