Evolution of a Novel, Orally Bioavailable Series of PI3Kδ Inhibitors from an Inhaled Lead for the Treatment of Respiratory Disease
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- 作者：Augustin Amour ; Nick Barton ; Anthony W. J. Cooper ; Graham Inglis ; Craig Jamieson ; Christopher N. Luscombe ; Josie Morrell ; Simon Peace ; David Perez ; Paul Rowland ; Chris Tame ; Sorif Uddin ; Giovanni Vitulli ; Natalie Wellaway
- 刊名：Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：August 11, 2016
- 年：2016
- 卷：59
- 期：15
- 页码：7239-7251
- 全文大小：587K
- 年卷期：0
- ISSN：1520-4804
文摘
A four-step process of high-quality modeling of existing data, deconstruction, identification of replacement cores, and an innovative synthetic regrowth strategy led to the rapid discovery of a novel oral series of PI3Kδ inhibitors with promising selectivity and excellent in vivo characteristics.