title: Inhibition of PCAF histone acetyltransferase and cytotoxic effect of N-acylanthranilic acids.
abstract: 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 μM. 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.
authors.affiliation: College of Pharmacy, Catholic University of Daegu, Hayang, 712-702, Korea.
authors.forename: Woong Jae
authors.initials: WJ
authors.lastname: Park
authors.forename: Eunsook
authors.initials: E
authors.lastname: Ma
mesh_terms: D048729:Anacardic Acids / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D013329:Structure-Activity Relationship; D062367:ortho-Aminobenzoates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D050880:p300-CBP Transcription Factors / Q000037:antagonists & inhibitors*; D000099224:p300-CBP-Associated Factor
chemical_list: D048729:Anacardic Acids; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D062367:ortho-Aminobenzoates; D050880:p300-CBP Transcription Factors; D000099224:p300-CBP-Associated Factor; C088115:anacardic acid