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Bioorg Med Chem Lett. 2008 Mar 15;18(6):1994-9. doi: 10.1016/j.bmcl.2008.01.119. Epub 2008 Feb 6.

Synthesis and SAR studies of indole-based MK2 inhibitors.

Author information

1
Research and Development, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, Ridgefield, CT 06877, USA. zhaoming.xiong@boehringer-ingelheim.com

Abstract

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.

PMID:
18291646
DOI:
10.1016/j.bmcl.2008.01.119
[Indexed for MEDLINE]

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