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Bioorg Med Chem Lett. 2006 Aug 15;16(16):4326-30. Epub 2006 Jun 2.

Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.

Author information

1
Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6100, USA. zhiqin.ji@abbott.com

Abstract

A series of isothiazolopyrimidines and isoxazolopyrimidines were synthesized and identified as potent KDR inhibitors. SAR studies led to isothiazolopyrimidine urea analogs that potently inhibit VEGFR tyrosine kinases (KDR enzymatic and cellular IC(50) values below 10 nM) as well as cKIT and TIE2. The selected compounds 8 and 13 display 56% and 48% oral bioavailability in mice, respectively.

PMID:
16735117
DOI:
10.1016/j.bmcl.2006.05.057
[Indexed for MEDLINE]

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