Journal: Pharmaceutics
Article Title: Generation and Characterization of Novel Contilisant+Tubastatin a Multitarget Small Molecules Against Glioblastoma
doi: 10.3390/pharmaceutics17121594
Figure Lengend Snippet: Novel FRB compounds present antitumor activity. ( A ) IC 50 values of FBR21, FRB24, FRB44 and FRB56 in the glioblastoma (U87), glioma (U251), patient-derived GSC (GNS166), primary human astrocyte (NHA), gastric cancer (MKN45), pancreatic cancer (RWP1) and lung cancer (H1299) cell lines measured by MTT. ( B ) WB of HDAC6 and its target (acetylated α-tubulin) in GNS166-treated cells and U87-treated cells. ( C ) HDAC6, acetylated α-tubulin, HDAC1, acetylated histone 3 and total acetylated lysine protein expression in FRB- and Tubastatin A-treated GNS166 cells and ( D ) U87 cells. ( E ) MAO-A and MAO-B inhibitory capacity of FRBs and reference compounds Clorgiline, Selegiline and Rasalgiline. ( F ) AChE and BChE inhibitory capacity of FRBs and reference compounds Donepezil and Rivastigmine. n.i.: No inhibition.
Article Snippet: U87-MG, U251-MG and NCI-H1299 cells were purchased from ATCC, while MKN45 was obtained from the Leibniz Institute DSMZ-German Collection of Microorganisms and Cell Cultures and the RWP1 cell line was kindly provided by Dr. Francisco Real.
Techniques: Activity Assay, Derivative Assay, Expressing, Inhibition