共激活因子相关精氨酸甲基转移酶1（CARM1）的苯并[d]咪唑抑制剂——从苗头化合物到先导化合物的研究
Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)--Hit to Lead studies.
作者信息
Wan Honghe, Huynh Tram, Pang Suhong, Geng Jieping, Vaccaro Wayne, Poss Michael A, Trainor George L, Lorenzi Matthew V, Gottardis Marco, Jayaraman Lata, Purandare Ashok V
机构信息
Bristol-Myers Squibb Pharmaceutical Research and Development, Princeton, NJ 08543, USA.
出版信息
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5063-6. doi: 10.1016/j.bmcl.2009.07.040. Epub 2009 Jul 10.
PMID:19632837
Abstract
Hit to Lead optimization and SAR development led to the identification of the potent and selective benzo[d]imidazole inhibitor (17b) of Co-activator Associated Arginine Methyltransferase (CARM1).
摘要
从命中化合物到先导化合物的优化以及构效关系（SAR）研究促成了强效且具选择性的共激活因子相关精氨酸甲基转移酶（CARM1）苯并[d]咪唑抑制剂（17b）的发现。
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