Novel 1,2,4-triazole derivatives as apoptotic inducers targeting p53: Synthesis and antiproliferative activity

Novel pyrrolizines bearing 3,4,5-trimethoxyphenyl moiety: design, synthesis, molecular docking, and biological evaluation as potential multi-target cytotoxic agents

“…The cytotoxic activity of our previously reported pyrrolizine-5-carboxamide 9a was mediated by the induction of apoptosis in MCF-7 cells 13,19 . Accordingly, compounds 16a,b,d, the most active in the MTT assay (Table 1) were selected to investigate their apoptosis-inducing activities.…”

“…The ability of compounds 16a , b , d to induce apoptotic changes in MCF-7 cells was determined by Annexin V-FITC/PI staining according to the previous report 13 , 18 , 19 . Additionally, the morphological changes in MCF-7 cells were examined by microscope.…”

“…CH-3 0 þCH-5 0 ). MS (EI): 19), 458 (M þ , 72), 457 (7), 429 (4), 353 (21), 352 (100), 336 (4), 322 (7), 308 (7), 292 (11) 4), 458 (7), 353 (13), 352 (73), 323 (4), 322 (8), 311 (11), 308 (10), 292 (12), 291 (44), 278 (8), 263 (13), 252 (9), 229 (8), 222 (11), 196 (15), 195 (100), 186 (20), 168 (28), 154 (12), 147 (6), 111 (4), 106 (5), 91 (7), 77 (12)…”

Recent advances in the chemistry of 1,2,4-triazoles: Synthesis, reactivity and biological activities

“…The development of original synthetic approaches for the preparation of fused 1,2,4-triazoles has received a great deal of interest because of their wide range of biological activities. 51 For examples, Hayallah, Youssif et al 52 Further, Ibrar et al 53 reported an efficient synthetic method to the synthesis of thiazolo [3,2-b][1,2,4]triazole derivatives and evaluated their urease inhibition potential. The sequence proceeds through coupling coumarinyl 3-mercapto-1,2,4triazole with substituted acetophenones to form the corresponding substituted ethanones which after treatment with phosphorus oxychloride were transformed to coumarinyl thiazolotriazoles (Scheme 36).…”

Synthesis and herbicidal activity of pyrimidyl‐1,2,4‐triazole derivatives containing aryl sulfonyl moiety

“…As a class of nitrogen-containing five-membered heterocyclic compounds, 1,2,4-triazoles play a crucial role in the development of agrochemicals and drug molecules due to their interesting structural features and outstanding biological properties, such as antioxidant [9], antiproliferative [10], antimicrobial [11], antifungal [12], antitubercular [13], anticancer [14], antiinflammatory [15], antiviral [16], anti-HIV [17], molluscicidal [18], and herbicidal [19]. Currently, many 1,2,4-triazole derivatives have been marketed as herbicides, including carfentrazone and flupoxam [20].…”