Most conventional anticancer drugs exert either anti-proliferation or anti-angiogenesis activity. Recently, searching for potential multi-target agents has become an alternative strategy for
cancer treatment. Several structurally different
carbazole alkaloids from either natural or synthesized sources represent an important and heterogeneous class of
anticancer agents. In the present study, we investigated the anticancer activity of a novel synthetic
carbazole derivative, 9-[(6-chloropyridin-4-yl)methyl]-9H-
carbazole-3-
carbinol (HYL-6d), which is structurally different from other previously characterized
carbazoles. HYL-6d-treated human
breast cancer MCF-7 cells exhibited an increased population arrested at the sub-G1 and S phases, as well as an increase of p53 and decrease of cyclin D1, A and CDK2. Also,
HYL-6d treatment induced MCF-7 cell apoptosis and this was accompanied by a decreased expression of Bcl-2, increased levels of p53 and Bcl-XS and the activation of
caspase-9. Experimental results from human umbilical vascular endothelial cells (HUVECs) showed that
HYL-6d also exerted its anti-angiogenic activity in HUVECs by inhibiting cell proliferation, migration, and tube formation induced by
VEGF- or bFGF in vitro. In summary, the data indicate that
HYL-6d exhibits both cytotoxic effects against human
cancer cells and anti-angiogenic activities, which make it a potential therapeutic drug for
cancer treatment.