50356-95-1Relevant academic research and scientific papers
Synthesis and evaluation of pyridinium-hydrazone derivatives as potential antitumoral agents
Parlar, Sülünay,Erzurumlu, Yal??n,Ilhan, Recep,Ballar K?rm?z?bayrak, Petek,Alptüzün, Vildan,Erciyas, Ercin
, p. 1198 - 1205 (2018)
The hydrazones of 4-hydrazinylpyridinium bearing alkylphenyl groups on pyridinium nitrogen were synthesized and evaluated for their cytotoxic activity against MCF-7, PC3, U2OS, and HEK293 cell lines by Wst1 cell proliferation assay. Cytotoxic activity results indicated that d derivatives having butylene chain; 4 and 5 series having naphthalene and anthracene ring systems showed high cytotoxic activity (IC50?=?3.27–8.54?μm) on cancer cells. 3d (4-(2-(4-hydroxybenzylidene)hydrazinyl)-1-(4-phenylbutyl)pyridinium bromide) was the most cytotoxic compound with IC50 value of 3.27?μm against MCF-7. The most active derivatives (1d, 2d, 3d, 4, and 5 series) were selected to investigate for the effects on autophagy by analyzing the expression of autophagy marker proteins. The conversion of LC3-I to its lipidated form LC3-II is essential for autophagy and related to autophagosomes. According to our results, all tested compounds except for 3d induced lipidated form LC3-II accumulation. Then, the effects of the compounds on p62 protein level were also analyzed by the immunoblotting as the autophagy inhibition results in accumulation of p62. Further molecular mechanistic studies including morphological analysis and live–death assays indicated that all tested compounds (1d, 2d, 3d, 4, and 5 series) are potent antitumoral molecules and all except for 3d have potential to inhibit autophagic flux.
Quinolylhydrazones as novel inhibitors of Plasmodium falciparum serine protease PfSUB1
Gemma, Sandra,Giovani, Simone,Brindisi, Margherita,Tripaldi, Pierangela,Brogi, Simone,Savini, Luisa,Fiorini, Isabella,Novellino, Ettore,Butini, Stefania,Campiani, Giuseppe,Penzo, Maria,Blackman, Michael J.
scheme or table, p. 5317 - 5321 (2012/09/07)
Plasmodium falciparum subtilisin-like protease 1 (PfSUB1) is a serine protease that plays key roles in the egress of the parasite from red blood cells and in preparing the released merozoites for the subsequent invasion of new erythrocytes. The development of potent and selective PfSUB1 inhibitors could pave the way to the discovery of potential antimalarial drugs endowed with an innovative mode of action and consequently able to overcome the current problems of resistance to established chemotherapies. Through the screening of a proprietary library of compounds against PfSUB1, we identified hydrazone 2 as a hit compound. Here we report a preliminary investigation of the structure-activity relationships for a class of PfSUB1 inhibitors related to our identified hit.
