Synthesis and evaluation of alkenyl indazoles as selective Aurora kinase inhibitors

Stéphanie Blanchard; Anthony D William; Angeline C-H Lee; Anders Poulsen; Ee Ling Teo; Weiping Deng; Noah Tu; Evelyn Tan; Kay Lin Goh; Wai Chung Ong; Chee Pang Ng; Kee Chuan Goh; Zahid Bonday; Eric T Sun

doi:10.1016/j.bmcl.2010.03.018

Synthesis and evaluation of alkenyl indazoles as selective Aurora kinase inhibitors

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2443-7. doi: 10.1016/j.bmcl.2010.03.018. Epub 2010 Mar 7.

Authors

Stéphanie Blanchard¹, Anthony D William, Angeline C-H Lee, Anders Poulsen, Ee Ling Teo, Weiping Deng, Noah Tu, Evelyn Tan, Kay Lin Goh, Wai Chung Ong, Chee Pang Ng, Kee Chuan Goh, Zahid Bonday, Eric T Sun

Affiliation

¹ S*BIO Pte. Ltd, The Capricorn, Singapore Science Park II, Singapore 117528, Singapore. stephanie_blanchard@sbio.com

PMID: 20338758
DOI: 10.1016/j.bmcl.2010.03.018

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.

MeSH terms

Aurora Kinases
Drug Evaluation, Preclinical
Models, Molecular
Protein Kinase Inhibitors / chemical synthesis*
Protein Kinase Inhibitors / chemistry
Protein Kinase Inhibitors / metabolism
Protein Kinase Inhibitors / pharmacology
Protein Serine-Threonine Kinases / antagonists & inhibitors*
Protein Serine-Threonine Kinases / metabolism

Substances

Protein Kinase Inhibitors
Aurora Kinases
Protein Serine-Threonine Kinases