An orally antitumor chalcone hybrid inhibited HepG2 cells growth and migration as the tubulin binding agent

SummaryLiver cancer is a kind of high mortality cancer due to the difficulty of early diagnosis. It is necessary to develop the anticancer agents to treat liver cancer. Here, a novel chalcone derivative was synthesized and evaluated for anticancer activity in vitro against liver cancer cell lines (HepG2, SNU-423, SMMC7221, and SNU-398). The chalcone hybrid9 displayed the antiproliferative effect against HepG2, SNU-423, SMMC7221 and SNU-398 cells with IC50 values of 0.9  μM, 2.7 μM, 6.2 μM and 4.6 μM, respectively. Cellular mechanisms showed that derivative9 could obviously inhibit HepG2 cells growth and colony formation in a concentration-dependent manner. Analogue9 inhibited the migration by regulating the expression levels of migration-releated markers and transcription factors (Snail and Slug). Tubulin polymerization inhibition assay illustrated that chalcone hybrid9 might be a potent tubulin polymerization inhibitor. Importantly, compound9 displayed the antitumor activity against liver cancer HepG2 cells in vivo with the low toxicity toward mice. Therefore, compound9 as a novel tubulin polymerization inhibitor deserves further investigation to treat liver cancer.Graphical abstractCompound9 displayed the antitumor activity against liver cancer HepG2 cells in vivo and low toxicity toward mice Figure: Orally antitumor chalcone hybrid 9 inhibited HepG2 cells growth and migration as the tubulin binding agent.
Source: Investigational New Drugs - Category: Drugs & Pharmacology Source Type: research