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Start Over Author "Ha Yeon Cho" Publisher american chemical society (acs)
1 results on '"Ha Yeon Cho"'

1. X-ray Crystal Structure-Guided Design and Optimization of 7H-Pyrrolo[2,3-d]pyrimidine-5-carbonitrile Scaffold as a Potent and Orally Active Monopolar Spindle 1 Inhibitor

Author

Seo Kyung Ah, Son Jung Beom, Ikyon Kim, Jun Goo Jee, Nam Doo Kim, Kim Hyunkyung, Haelee Kim, Eunhwa Ko, Hwan Geun Choi, Younho Lee, and Ha Yeon Cho

Subjects
0303 health sciences, Scaffold, Pyrimidine, Crystal structure, Tnbc cell, 01 natural sciences, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, 03 medical and health sciences, chemistry.chemical_compound, Orally active, chemistry, In vivo, Drug Discovery, Cancer research, Molecular Medicine, Protein kinase A, Monopolar spindle, 030304 developmental biology
Abstract

Triple-negative breast cancer (TNBC) is an aggressive breast-cancer subtype associated with poor prognosis and high relapse rates. Monopolar spindle 1 kinase (MPS1) is an apical dual-specificity protein kinase that is over-expressed in TNBC. We herein report a highly selective MPS1 inhibitor based on a 7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile scaffold. Our lead optimization was guided by key X-ray crystal structure analysis. In vivo evaluation of candidate (9) is shown to effectively mitigate human TNBC cell proliferation.

Published
2021
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