期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 6, 页码 1994-1999出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.01.119
关键词
MAPKAP-k2; MK2; beta-carbolinone; pyrazino[1,2-a] indolone; diazepino[1,2-a]indolone
Chemistry has been developed to specifically functionalize two structurally similar classes of indole-based MK2 inhibitors at positions prompted by a combination of X-ray crystallographic and computer assisted drug design. A gain in molecular potency was obtained by introducing aminomethyl groups to the lactam rings of 6-arylcarbamoyl-tetrahydro-beta-carbolinone and 6-arylcarbamoyl-dihydropyrazino[1,2-a] indolone MK2 inhibitors. In addition, improvements in molecular potency were achieved by expansion of the lactam from a 6- to 7-membered ring leading to 7-arylcarbamoyl-tetrahydro-[1,4] diazepino[1,2-a]indolones. (C) 2008 Elsevier Ltd. All rights reserved.
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