916522-82-2Relevant academic research and scientific papers
Synthesis and SAR studies of indole-based MK2 inhibitors
Xiong, Zhaoming,Gao, Donghong Amy,Cogan, Derek A.,Goldberg, Daniel R.,Hao, Ming-Hong,Moss, Neil,Pack, Edward,Pargellis, Chris,Skow, Donna,Trieselmann, Thomas,Werneburg, Brian,White, Andre
, p. 1994 - 1999 (2008/09/21)
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.
