Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: Potent Inhibitors of the IGF-1R Receptor Tyrosine Kinase

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2008 Dec 6

PMID 19056263

Citations 4

Authors

Stanley D Chamberlain

Joseph W Wilson

Felix DeAnda

Samarjit Patnaik

Aniko M Redman

Bin Yang

Lisa Shewchuk

Peter Sabbatini

M Anthony Leesnitzer

Arthur Groy

Charity Atkins

Roseanne Gerding

Anne M Hassell

Huangshu Lei

Robert A Mook Jr

Ganesh Moorthy

Jason L Rowand

Kirk L Stevens

Rakesh Kumar

J Brad Shotwell

Affiliations

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Abstract

The evaluation of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines as inhibitors of the IGF-1R (IGF-IR) receptor tyrosine kinase is reported. Examples demonstrate nanomolar potencies in in vitro enzyme and mechanistic cellular assays as well as promising in vivo pharmacokinetics in rat.

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