Synthesis and antiproliferative evaluation of amide-containing anthraquinone, xanthone, and carbazole

Article abstract of DOI:10.1248/cpb.c13-00617

Certain amide-containing anthraquinone, xanthone, and carbazole derivatives have been synthesized and evaluated in vitro for their antiproliferative activities against a panel of human cancer cell lines including nasopharyngeal carcinoma (NPC-TW01), lung carcinoma (NCI-H661), and leukemia (Jurkat). Among them, 2-(9,10-dioxo-9,10-dihydroanthracen-2-yloxy)-N-(naphthalen-2-yl)acetamide (13) was the most active against NPC-TW01 with an IC₅₀ value of 2.62 μM while its xanthone and dibenzofuran counterparts, 14 and 15, were inactive with an IC₅₀ value of 16.10 and 11.09 μM, respectively. Studies on NPC-TW01 cell cycle distribution revealed that compound 13 inhibited proliferation of NPC-TW01 by the alteration of cell division and the accumulation of cells in G₀/G₁ phase.