Synthesis and cytotoxicity evaluation of N-(5-Mercapto-4H-1,2,4-triazol-3-yl)-2-phenylacetamide derivatives as apoptosis inducers with potential anticancer effects

An Efficient Synthesis of 1-(1,3-Dioxoisoindolin-2-yl)-3-aryl Urea Analogs as Anticancer and Antioxidant Agents: An Insight into Experimental and In Silico Studies

“…Similarly, the structure–activity relationship against the EKVX and MCF7 cell lines are shown in Figure 2 . The replacement of the NH function with CH 2 increased the anticancer activity against PC3 and HT29 as evidenced from previous reported work [ 48 ]. Previous reports have demonstrated a decrease in anticancer activity against PC3 and HT29 when the NH function was replaced with CH 2 together with the replacement of the phenyl ring with the bulky benzylthio-1,3,4-thiadiazole moiety [ 49 ].…”

Investigation of novel bis-thiadiazole bearing schiff base derivatives as effective inhibitors of thymidine phosphorylase: Synthesis, in vitro bioactivity and molecular docking study

“…In order to synthesize (2E,2′E)-2,2′-(pyridine-2,6-diylbis(methanylylidene))bis(hydrazine-1-carbothioamide) as an intermediate ( 2 ), pyridine-2,6-dicarbaldehyde ( 1 ) was mixed with hydrazinecarbothioamide (two molar), which was then refluxed in MeOH along with addition of CH 3 COOH as a catalyst. This reaction was then allowed to run on reflux for 6 h. Further, (2E,2′E)-2,2′-(pyridine-2,6-diylbis(methanylylidene))bis(hydrazine-1-carbothioamide) substrate underwent oxidative cyclization with I 2 and K 2 CO 3 using 1,4-dioxane to afford 5,5′-(pyridine-2,6-diyl)bis(1,3,4-thiadiazol-2-amine) as substrate ( 3 ) ( Aliabadi et al, 2017 ). In the last step, intermediate ( 3 ) was put in stirring and reflux with the different benzaldehyde derivatives in methanol and a catalytic amount of CH 3 COOH.…”

“…Molecular iodine (1 equivalent) was taken in round bottom flask using 1,4-dixoane (10 mL) as solvent, then ( 2E,2′E )-2,2′-(pyridine-2,6-diylbis(methanylylidene))bis(hydrazine-1-carbothioamide) ( 2 , 1 equivalent) and potassium carbonate (catalyst) were added to reaction mixture and stirred under refluxed 20 h. The solvent was extracted under decreased pressure after being cooled to 25 °C. The product ( 3 ) so obtained was precipitated, filtered, washed, dried and preserved for next reaction ( Aliabadi et al, 2017 ).…”