| Literature DB >> 20817449 |
Kevin K-C Liu1, Shubha Bagrodia, Simon Bailey, Hengmiao Cheng, Hui Chen, Lisa Gao, Samantha Greasley, Jacqui E Hoffman, Qiyue Hu, Ted O Johnson, Dan Knighton, Zhengyu Liu, Matthew A Marx, Mitchell D Nambu, Sacha Ninkovic, Bernadette Pascual, Kristina Rafidi, Caroline M-L Rodgers, Graham L Smith, Shaoxian Sun, Haitao Wang, Anle Yang, Jing Yuan, Aihua Zou.
Abstract
Pteridinones were designed based on a non-selective kinase template. Because of the uniqueness of the PI3K and mTOR binding pockets, a methyl group was introduced to C-4 position of the peteridinone core to give compounds with excellent selectivity for PI3K and mTOR. This series of compounds were further optimized to improve their potency against PI3Kα and mTOR. Finally, orally active compounds with improved solubility and robust in vivo efficacy in tumor growth inhibition were identified as well.Entities:
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Year: 2010 PMID： 20817449 DOI： 10.1016/j.bmcl.2010.08.045
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823