Abstract:
Cinnamyl- and thiazole-based compounds have been shown to exhibit diverse medicinal properties
and a series of twelve (E)-2-styrylthiazole and (E)-2-[(naphthalen-1-yl)vinyl]thiazole derivatives,
which are conjugates of both systems and which satisfy the “Lipinski rule of 5”, have been
synthesised and subjected to in vitro biological screening. While insignificant inhibition (60-98%
viability at 10 μM) of HeLa (cervical cancer) cells was noted, all five of the (E)-2-[naphthalen-1-
yl)vinyl]thiazole derivatives proved remarkably active against SH-SY5Y (neuroblastoma) cells
with IC50 values ranging from 2.09 to 8.64 μM. Two of the seven (E)-2-styrylthiazoles were found
to be moderately active (with IC50 values of 10.8 and 11.7 mM), whereas the remaining five
analogues exhibit significant proliferation of SH-SY5Y cells (with IC50 values of 180-1000 mM).
The results warrant further studies on the effects of styrylthiazoles on the differentiation and
extension of SH-SY5Y cells in order to assess their activity in neurological degenerative diseases.
