Synthesis and Screening of Novel Hybrid Benzothiazoles in U-87 MG Glioblastoma Cell Line

Abstract

Benzothiazole is a heteroaromatic compound known for its wide range of bioactivities including anti-cancer, anti-viral, anti-microbial, anti-inflammatory, anti-convulsant, anti-diabetic, anti-helminthic, and anti-tubercular activities. Research has shown that derivatives of benzothiazole exhibit inhibition of proliferation via apoptosis in various human cancer cell lines, such as liver cancer (Wang, et. al., 2011). In this study, a series of novel hybrid benzothiazole α-cyanostilbene derivatives and styrylbenzothiazole derivatives containing boronic acid and non-boronic acid pharmacophores were synthesized. The anti-cancer and anti-invasive properties of selected benzothiazole α-cyanostilbene derivatives on U-87MG glioblastoma cells were investigated in vitro. U-87MG cells were incubated with synthesized novel hybrid compounds at varying concentration to determine the lethal concentration 50 (LC50) of the compounds. All hybrid compounds displayed inhibitory effects on cell growth and the LC50 of the compounds varied depending on the nature of the pharmacophores. Moreover, compounds containing both boronic acid substituent and fluoro substituent exhibit lower LC50 than those that contain only one of the substituents. Cell motility has been investigated and we have found that was were no difference in motility between the treated and untreated cells. Results indicate anti-invasive properties in boronic acid and fluoro substituents at ortho position and boronic acid substituent at para position.