| Literature DB >> 20427182 |
Yongchun Shen1, Hong Du, Makoto Kotake, Tomohiro Matsushima, Masaki Goto, Hiroshi Shirota, Fabian Gusovsky, Xiangyi Li, Yimin Jiang, Shawn Schiller, Mark Spyvee, Heather Davis, Zhiyi Zhang, Robert Pelletier, Megumi Ikemori-Kawada, Yoshiyuki Kawakami, Atsushi Inoue, Yuan Wang.
Abstract
The potent in vitro lead compound, ER-803064 (2), a MEK1 and MEKK1 inhibitor inspired from natural product LL-Z1640-2 (f152A1), was further optimized to improve in vitro and in vivo potency. The modifications on C14 position led to discovery of the lead compounds 28 and 29, which regained full in vitro potency of f152A1 and showed higher in vivo potency by iv administration. Copyright 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20427182 DOI： 10.1016/j.bmcl.2010.03.119
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823