| Literature DB >> 30715878 |
Xiaojing Wang1, Wesley Blackaby2, Vivienne Allen2, Grace Ka Yan Chan1, Jae H Chang1, Po-Chang Chiang1, Coura Diène2, Jason Drummond1, Steven Do1, Eric Fan1, Eric B Harstad1, Alastair Hodges2, Huiyong Hu1, Wei Jia1, William Kofie2, Aleksandr Kolesnikov1, Joseph P Lyssikatos1, Justin Ly1, Mizio Matteucci2, John G Moffat1, Veerendra Munugalavadla1, Jeremy Murray1, David Nash2, Cameron L Noland1, Geoff Del Rosario1, Leanne Ross1, Craig Rouse2, Andrew Sharpe2, Dionysos Slaga1, Minghua Sun1, Vickie Tsui1, Heidi Wallweber1, Shang-Fan Yu1, Allen J Ebens1.
Abstract
Pim kinases have been targets of interest for a number of therapeutic areas. Evidence of durable single-agent efficacy in human clinical trials validated Pim kinase inhibition as a promising therapeutic approach for multiple myeloma patients. Here, we report the compound optimization leading to GDC-0339 (16), a potent, orally bioavailable, and well tolerated pan-Pim kinase inhibitor that proved efficacious in RPMI8226 and MM.1S human multiple myeloma xenograft mouse models and has been evaluated as an early development candidate.Entities:
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Year: 2019 PMID： 30715878 DOI： 10.1021/acs.jmedchem.8b01857
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446