DW2282 [(S)-(+)-4-phenyl-1-[N-(4-aminobenzoyl) indoline-5-sulfonyl]-4,5-dih
ydro-2-imidazolone] hydrochloride] was derived from diarylsulfonylurea and
was identified as a prominent new anticancer agent. We examined the charact
eristics of DW2282 activity on the proliferation of human lung carcinoma ce
lls, A549 and human leukemic cells, K562. DW2282 effectively inhibited canc
er cell proliferation in vitro. Colony forming assay and viability tests de
monstrated that DW2282 is a cytotoxic agent rather than a cytostatic agent.
The isotope uptake test exhibited that DW2282 inhibited or inactivated pro
tein synthesis. Also, under conditions which cause RNA or protein synthesis
inhibition, by co-treatment with actinomycin D or cycloheximide, reduced t
he anticancer effects of DW2282. This means that the cytotoxicity of DW2282
depends partially on RNA or protein synthesis and proteins affected by DW2
282 may inactivate ol alter the process of the synthesis of another protein
. DW2282 activity was highly diminished in the presence of colcemid, a meta
phase spindle blocker. This result suggests that DW2282 may be related to t
he cell cycle. After exposure to DW2282, morphologically apoptotic cells ap
peared in A549 cells and fragmented DNA was detected in K562 cells. It demo
nstrated that apoptosis is one of the mechanisms by which DW2282 inhibits t
he proliferation of A549 and K562 cells.