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2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924 by Mark G. Saulnier; David B. Frennesson; Mark D. Wittman; Kurt Zimmermann; Upender Velaparthi; David R. Langley; Charles Struzynski; Xiaopeng Sang; Joan Carboni; Aixin Li; Ann Greer; Zheng Yang; Praveen Balimane; Marco Gottardis; Ricardo Attar; Dolatrai Vyas is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is 2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924 about?

A series of IGF-1R inhibitors is disclosed, wherein the (m-chlorophenyl)ethanol side chain of BMS-536924 (1) is replaced with a series of 2-(1H-imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chains. Some analogs show improved IGF-1R potency and oral exposure. Analogs from both series, 16a and 17f, show in vivo activity comparable to 1 in our constitutively activated IGF-1R Sal tumor model. This may be the due to the improved protein binding in human and mouse serum for imidazole 16a and the excellent oral exposure of pyrazole 17f.

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Author

Mark G. Saulnier; David B. Frennesson; Mark D. Wittman; Kurt Zimmermann; Upender Velaparthi; David R. Langley; Charles Struzynski; Xiaopeng Sang; Joan Carboni; Aixin Li; Ann Greer; Zheng Yang; Praveen Balimane; Marco Gottardis; Ricardo Attar; Dolatrai Vyas

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

2008

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)