期刊
ARCHIVES OF PHARMACAL RESEARCH
卷 35, 期 8, 页码 1379-1386出版社
PHARMACEUTICAL SOC KOREA
DOI: 10.1007/s12272-012-0807-2
关键词
Histone acetyltransferase (HAT); p300/CBP associated factor (PCAF); Cytotoxicity; N-Acylanthranilic acid
Small molecule HAT inhibitors are useful tools to unravel the role of histone acetyltransferases (HATs) in the cell and have relevance for oncology. We synthesized a series of N-acylanthranilic acids (11-16) and of N-acyl-5-hydroxyanthranilic acids (17-22) bearing C6, C8, C10, C12, C14, along with C16 acyl chain at the 2-amino position of anthranilic acid or 5-hydroxyanthranilic acid. Enzyme inhibition of these compounds was investigated, using in vitro PCAF HAT assays. All synthesized compounds (65-76%) showed similar inhibitory activity to anacardic acid (68%) at 100 mu M. The cytotoxicity, against one normal cell line (HSF) and eight cancer cell lines (HT-29, HCT-116, MDA-231, A-549, Hep3B, Caski, HeLa and Caki), were evaluated by the SRB method.
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