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Synthesis and Screening of N-Alkyl Hydroxamates for Inhibition of Cancer Cell Proliferation

[ Vol. 9 , Issue. 9 ]

Author(s):

Keith J. Stanger, Daniel Sliva, Jiahua Jiang and Viktor Krchnak   Pages 651 - 661 ( 11 )

Abstract:


A small library of N-alkylated amino acid-derived sulfonamide hydroxamates was synthesized on solid phase and tested for inhibition of proliferation of the highly invasive breast cancer cell line MDA-MB-231. The most active compound 4317 inhibited cell growth at IC50 30 μM. N-alkylation of N-H hydroxamate-based MMP inhibitors, a modification known to eliminate MMP activity, enhanced cell proliferation inhibition potency.

Keywords:

MMP inhibitors, N-alkylation, Gly-derived hydroxamates, invasive breast cancer cells, pyridine derivative

Affiliation:

Department of Chemistry and Biochemistry, 251 Nieuwland Science Center, University of Notre Dame,Notre Dame, IN 46556, USA.



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