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Small Molecule Caspase Inhibitors Using Isatin and Oxindole Scaffolds and a Combinatorial Approach

Abdallah, Hagar Mahmoud

Abstract Details

2010, Master of Science (MS), Wright State University, Chemistry.
Quinolyl-valyl-O-methylaspartyl-[2,6-difluorophenoxy]-methyl ketone (Q-VD-OPh) is a next generation broad spectrum caspase inhibitor, the effectiveness and reduced toxicity of which can be partially attributable to the carboxyterminal O-phenoxy group as well as the amino terminal quinolyl groups. We seek to incorporate some of these unique recognition elements onto small molecule derived protease inhibitors with drug like properties. Specifically, heterocyclic scaffolds such as isatins and oxindoles. Thus, isatins bearing electron withdrawing groups on C-5 and 2,6-difluorobenzyl moieties have been prepared by analogy to the well studied N-substituted 5-pyrrololidinylsulfonyl isatins. Moreover, 3-benzylidene oxindole derivatives bearing these structural motifs have also been prepared and their effectiveness as apoptosis inhibitors was examined employing human Jurkat T cells.
Daniel Ketcha, PhD (Advisor)
Kenneth Turnbull, PhD (Committee Member)
Eric Fossum, PhD (Committee Member)
91 p.

Recommended Citations

Citations

  • Abdallah, H. M. (2010). Small Molecule Caspase Inhibitors Using Isatin and Oxindole Scaffolds and a Combinatorial Approach [Master's thesis, Wright State University]. OhioLINK Electronic Theses and Dissertations Center. http://rave.ohiolink.edu/etdc/view?acc_num=wright1292600063

    APA Style (7th edition)

  • Abdallah, Hagar. Small Molecule Caspase Inhibitors Using Isatin and Oxindole Scaffolds and a Combinatorial Approach. 2010. Wright State University, Master's thesis. OhioLINK Electronic Theses and Dissertations Center, http://rave.ohiolink.edu/etdc/view?acc_num=wright1292600063.

    MLA Style (8th edition)

  • Abdallah, Hagar. "Small Molecule Caspase Inhibitors Using Isatin and Oxindole Scaffolds and a Combinatorial Approach." Master's thesis, Wright State University, 2010. http://rave.ohiolink.edu/etdc/view?acc_num=wright1292600063

    Chicago Manual of Style (17th edition)