Autor: |
Sunghoon Ma, Julie Lougheed, Christopher Jaeger, Scott W. Womble, Jean-Claire Limun Manalo, Chris A. Buhr, Longcheng Wang, Wentao Zhang, Kenneth D. Rice, Steven Charles Defina, Abigail R. Kennedy, Timothy S. Heuer, Michael Yakes, Neel Kumar Anand, Tae-Gon Baik, Curtis Jeff Kimo, Joerg Bussenius, Angie I. Kim, Jonathan C. Li, Michael Pack, Csaba J. Peto, Monique Nicoll, Naing Aay, Simona Costanzo, Jae Lee, Garth Joseph Mcgrath, Charles M. Blazey, Tsze H. Tsang, Shiva Malek, Anagha Abhijit Joshi, Arlyn Arcalas, Ping Huang, Larisa Dubenko, Jean-Francois Martini, Katherine Lara, John M. Nuss, Owen Joseph Bowles |
Rok vydání: |
2012 |
Předmět: |
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Zdroj: |
Bioorganic & Medicinal Chemistry Letters. 22:5396-5404 |
ISSN: |
0960-894X |
Popis: |
With structural guidance, tropane-derived HTS hits were modified to optimize for HSP90 inhibition and a desirable in vivo profile. Through an iterative SAR development process 12i (XL888) was discovered and shown to reduce HSP90 client protein content in PD studies. Furthermore, efficacy experiments performed in a NCI-N87 mouse xenograft model demonstrated tumor regression in some dosing regimens. |
Databáze: |
OpenAIRE |
Externí odkaz: |
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