381197-10-0Relevant academic research and scientific papers
Antitumor activity of (-)-α-bisabolol-based thiosemicarbazones against human tumor cell lines
Da Silva, Alan P.,Martini, Manuele V.,De Oliveira, Cecília M.A.,Cunha, Silvio,De Carvalho, Jo?o E.,Ruiz, Ana L.T.G.,Da Silva, Cleuza C.
experimental part, p. 2987 - 2993 (2010/08/22)
A series of thiosemicarbazones deriving from the natural sesquiterpene (-)-α-bisabolol were synthesized and tested against a panel of eight human tumor cell lines to evaluate their anti-tumor potential. Some of the compounds exhibited inhibitory effects on the growth of a wide range of cancer cell lines, but myeloid leukemia cells (K-562) were especially sensitive to all tested thiosemicarbazones (GI50 0.01-4.22 μM). Among the analogues, the ketone derivative 3l was the most active, exhibiting potent antitumoral activity (GI50 0.01 μM) and high selectivity for K-562 cells (δTGI 505). It also demonstrated high cytotoxicity, with an LC50 of 1.55 μM for the K-562 cells, but it showed only moderate selectivity (δLC50 38.5 μM). Through structure-activity relationship studies, we identified some structural requirement for the antitumoral activity exhibited by these promising compounds.
