Olawode, Emmanuel O.Tandlich, RomanPrinsloo, EarlIsaacs, MichelleHoppe, HeinrichSeldon, RonnettWarner, Digby F.Steenkamp, VanessaKaye, Perry T.2017-11-202017-11-202017-04Olawode, E.O. et al. 2017, 'Synthesis and biological evaluation of (E)-cinnamic acid, (E)-2-styrylthiazole and (E)-2-[2-(naphthalen-1-yl)vinyl]thiazole derivatives', Arkivoc, Part vi. pp. 284-296.1551-7012 (print)1551-7004 (online)10.3998/ark.5550190.p009.905http://hdl.handle.net/2263/63240Cinnamyl- 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.en© ARKAT-USA, Inc. Published with a Creative Commons Attribution Non-Commercial License.SynthesisCinnamic acidsStyrylthiazoles2-[2-(Naphthalen-1-yl)vinyl]thiazolesBiological activityPeptidesPlasmodium falciparumArticle