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Synthesis and evaluation of alkenyl indazoles as selective Aurora kinase inhibitors
Authors: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
Affiliation:S1BIO Pte. Ltd, 1 Science Park Road, #05-09 The Capricorn, Singapore Science Park II, Singapore 117528, Singapore
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.
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