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

Author(s): Keith J. Stanger, Daniel Sliva, Jiahua Jiang, Viktor Krchnak.

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Volume 9 , Issue 9 , 2006

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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

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Article Details

Year: 2006
Page: [651 - 661]
Pages: 11
DOI: 10.2174/138620706778700161
Price: $58

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