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Presentation
Utilization of Triazine Scaffolds as Potential Caspase Inhibitors Related to Q-VD-OPH
Abstracts of Papers - American Chemical Society
  • Patrick Seymour
  • William C. Grunwald, Jr., Wright State University - Main Campus
  • Kashmira Kulkarni
  • David R. Cool, Wright State University - Main Campus
  • Thomas L. Brown, Wright State University - Main Campus
  • Daniel M. Ketcha, Wright State University - Main Campus
Document Type
Presentation
Publication Date
4-1-2008
Abstract

Quinolyl-valyl-O-methylaspartyl-[-2,6-difluorophenoxy]methyl ketone (Q-VD(OMe)-OPH) is a next generation broad spectrum caspase inhibitor with potential promise as a therapeutic agent. In seeking to both reduce the peptidic features and increase the efficacy of caspase inhibitors, we have chosen to examine derivatives based upon the triazine scaffold. The typical protocol for rapid analog synthesis upon this scaffold involves the initial introduction of an aryl amine, followed by substitution at the secondary site by a more nucleophilic amine input. Finally, introduction of the third amine input usually requires extended heating. So as to avert this heating step we have elected to instead utilize the introduction of two oxygen-based nucleophiles followed by addition of the aspartyl phenoxy methyl ketone warhead portion.

Comments

Poster presented at the 235th American Chemical Society (ACS) National Meeting, New Orleans, LA.

Citation Information
Patrick Seymour, William C. Grunwald, Kashmira Kulkarni, David R. Cool, et al.. "Utilization of Triazine Scaffolds as Potential Caspase Inhibitors Related to Q-VD-OPH" Abstracts of Papers - American Chemical Society Vol. 235 (2008) ISSN: 0065-7727
Available at: http://works.bepress.com/thomas_brown/49/