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Structure-based Optimization of MurF Inhibitors

✍ Scribed by Geoffrey F. Stamper; Kenton L. Longenecker; Elizabeth H. Fry; Clarissa G. Jakob; Alan S. Florjancic; Yu-Gui Gu; David D. Anderson; Curt S. Cooper; Tianyuan Zhang; Richard F. Clark; Yingna Cia; Candace L. Black-Schaefer; J. Owen McCall; Claude G. Lerner; Philip J. Hajduk; Bruce A. Beutel; Vincent S. Stoll

Book ID
111368240
Publisher
John Wiley and Sons
Year
2006
Tongue
English
Weight
566 KB
Volume
67
Category
Article
ISSN
1747-0277

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In this Letter is described the structure-based design of potent dihydro-pyrazoloquinazolines as PDK1 inhibitors. Starting from low potency HTS hits with the aid of X-ray crystallography and modeling, a medicinal chemistry activity was carried out to improve potency versus PDK1 and selectivity versu