| Literature DB >> 21353551 |
Andrew P Crew1, Shripad V Bhagwat, Hanqing Dong, Mark A Bittner, Anna Chan, Xin Chen, Heather Coate, Andrew Cooke, Prafulla C Gokhale, Ayako Honda, Meizhong Jin, Jennifer Kahler, Christine Mantis, Mark J Mulvihill, Paula A Tavares-Greco, Brian Volk, Jing Wang, Douglas S Werner, Lee D Arnold, Jonathan A Pachter, Robert Wild, Neil W Gibson.
Abstract
The discovery and optimization of a series of imidazo[1,5-a]pyrazine inhibitors of mTOR is described. HTS hits were optimized for potency, selectivity and metabolic stability to provide the orally bioavailable proof of concept compound 4c that demonstrated target inhibition in vivo and concomitant inhibition of tumor growth in an MDA-MB-231 xenograft model.Entities:
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Year: 2011 PMID： 21353551 DOI： 10.1016/j.bmcl.2011.01.139
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823