Synthesis and toxicological evaluation using brine shrimp lethality assay of novel 1,2,4-triazole derivatives with anticancer activity

1,2,4-triazole derivatives are recognized to possess various biological activities as antiparasitic, antifungal, antimicrobial and antiproliferative. The present work reports the synthesis of six new derivatives under microwave irradiation with the purpose of developing new drugs that present high specificity for tumor cells and low toxicity to the organism. The synthesized compounds were characterized by IR, 1H-NMR, and mass spectral data. The present studies widen the scope of the brine shrimp model that may prove quite helpful as a preliminary screen in the anticancer drug designing and synthesis expeditions. In Brine shrimp lethality bioassay, compounds produced dose dependent cytotoxicity effect to brine shrimp nauplii. All the newly synthesized compounds 2a-f were further evaluated for anticancer activity against MCF-7 cell lines using MTT assay and compound 2d could be considered as possible hit as therapeutic agents. The study draws a very good relationship between a simple, inexpensive, and bench-top BSL assay and the antitumor potential of the cytotoxic compounds.