受瑞香素 LL-Z1640-2 启发的抗炎临床候选药物 E6201 的发现，III。
Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III.
机构信息
Eisai Inc., Andover, MA 01810, USA.
出版信息
Bioorg Med Chem Lett. 2010 May 15;20(10):3155-7. doi: 10.1016/j.bmcl.2010.03.087. Epub 2010 Mar 30.
PMID:20399648
Abstract
Inspired by natural product, LL-Z1640-2, clinical candidate, E6201 (22) was discovered in a medicinal chemistry effort through total synthesis. The modification on C14-position to N-alkyl substitution showed to be potent in vitro and orally active in vivo in anti-inflammatory assays.
摘要
受天然产物启发，临床候选药物 LL-Z1640-2 的前药 E6201（22）通过全合成在药物化学研究中被发现。C14 位的 N-烷基取代修饰在抗炎试验中显示出体外强效和体内口服活性。
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