1.
Bioorg Med Chem Lett
; 18(6): 1916-21, 2008 Mar 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18308565
RESUMO
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.