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Bioorg Med Chem Lett. 2010 Jan 1;20(1):153-6. doi: 10.1016/j.bmcl.2009.11.021. Epub 2009 Nov 12.

A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors.

Author information

1
Vertex Pharmaceuticals Inc., 130 Waverly St., Cambridge, MA 02139-4242, United States. tiansheng_wang@vrtx.com

Erratum in

  • Bioorg Med Chem Lett. 2010 Apr 15;20(8):2684. Salituro, Francesco G [added].

Abstract

Pictet-Spengler condensation of aldehydes or alpha-keto-esters with 4-(2-anilinophenyl)-7-azaindole (11) or deazapurine (12) gave high yields of the 3,4-fused cyclic compounds. SAR studies, by varying the substituted benzaldehyde components, lead to the discovery of a series of potent JAK2 kinase inhibitors.

PMID:
19945871
DOI:
10.1016/j.bmcl.2009.11.021
[Indexed for MEDLINE]

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