Bioorg Med Chem Lett. 2010 Apr 15;20(8):2443-7. Epub 2010 Mar 7.

Synthesis and evaluation of alkenyl indazoles as selective Aurora kinase inhibitors.

Blanchard S, William AD, Lee AC, Poulsen A, Teo EL, Deng W, Tu N, Tan E, Goh KL, Ong WC, Ng CP, Goh KC, Bonday Z, Sun ET.

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S*BIO Pte. Ltd, The Capricorn, Singapore Science Park II, Singapore 117528, Singapore. stephanie_blanchard@sbio.com

Abstract

A series of alkenyl indazoles were synthesized and evaluated in Aurora kinase enzyme assays. Several promising leads were optimized for selectivity towards Aurora B. Excellent binding affinity and good selectivity were achieved with optimized compounds in isolated Aurora subfamily assays.

PMID:: 20338758; [PubMed - indexed for MEDLINE]

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