Synthesis and In vitro Antiproliferative Activity of 5-Halogen-6-nitrobenzo[c][1,2,5]selenadiazoles on A549 Cells.

Selenadiazoles are of a broad spectrum of promising anticancer agents. However, excessive synthetic steps, larger molecular size and erratic anticancer activity involve. In this work, three 5-halogen-6-nitrobenzo[c][1,2,5]selenadiazoles with fairly small size were synthesized by only one step and their structure was characterized by MS-ESI and NMR. In vitro anticancer activity showed that they exerted significant antiproliferative activity against various tumor cells. Compound 1c exhibited the best antiproliferative effect on A549 cells. Furthermore, (Ic) significantly inhibited the colony formation, migration and invasion of A549 cells, arrested the cell cycle in G0/G1 phase by down-regulating the expression levels of Cyclin A1, Cyclin E and CDK1, induced cell apoptosis by up-regulating the expression levels of P21, Bax, Cleaved-Caspase-7 and Cleaved-Caspase-8, as well as Cleaved PARP1. [ABSTRACT FROM AUTHOR]