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

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

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

Affiliation

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

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

Article in En | MEDLINE | ID: mdl-20338758

ABSTRACT

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.

Subject(s)

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

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Full text: 1 Database: MEDLINE Main subject: Protein Serine-Threonine Kinases / Protein Kinase Inhibitors Language: En Year: 2010 Type: Article

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Full text: 1 Database: MEDLINE Main subject: Protein Serine-Threonine Kinases / Protein Kinase Inhibitors Language: En Year: 2010 Type: Article