Synthesis and SAR studies of indole-based MK2 inhibitors.
Bioorganic & Medicinal Chemistry Letters(2008)
摘要
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-β-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.
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关键词
MAPKAP-k2,MK2,β-Carbolinone,Pyrazino[1,2-a]indolone,Diazepino[1,2-a]indolone
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