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AbstractA series of N‐(4‐cyano‐3‐trifluoromethyl‐phenyl)‐2‐ethoxy‐6‐alkyl (and alkenyl) benzamides related to the anacardic acid derivative CTPB have been prepared from 2,6‐dihydroxybenzoic acid with a Suzuki coupling and addition of the anion of 4‐cyano‐3‐trifluoromethylphenylamine to a benzodioxinone as the key steps. In U937 cells, these analogues, in particular 7 c, 7 d, 7 f and 7 j, induced cell‐cycle arrest in the G1 phase, caused apoptosis in about 20 % of the cells, and increased the acetylation levels of H3. These activities correlate with the enzymatic activation of histone lysine acetyltransferases (KATs): CBP and PCAF.
FP7, EC, Organic Chemistry, SP1-Cooperation, G1 Phase, Acetylation, Antineoplastic Agents, Apoptosis, Anacardic Acids, Health, Cell Line, Tumor, Benzamides, Molecular Medicine, Humans, General Pharmacology, Toxicology and Pharmaceutics, European Commission, Histone Acetyltransferases
FP7, EC, Organic Chemistry, SP1-Cooperation, G1 Phase, Acetylation, Antineoplastic Agents, Apoptosis, Anacardic Acids, Health, Cell Line, Tumor, Benzamides, Molecular Medicine, Humans, General Pharmacology, Toxicology and Pharmaceutics, European Commission, Histone Acetyltransferases
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