These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Synthesis and SAR studies of indole-based MK2 inhibitors.
    Author: Xiong Z, Gao DA, Cogan DA, Goldberg DR, Hao MH, Moss N, Pack E, Pargellis C, Skow D, Trieselmann T, Werneburg B, White A.
    Journal: Bioorg Med Chem Lett; 2008 Mar 15; 18(6):1994-9. PubMed ID: 18291646.
    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.
    [Abstract] [Full Text] [Related] [New Search]