Background: Triazine ring is a prominent structural motif found in some azanucleosides whose
efficiency improved many times in the research area of antitumor agents.
Objective: In this study, we have designed and synthesized novel 2-[(5,6-diphenyl-1,2,4-triazin-3-yl)thio]-N-(6-
substituted benzo/(thiazol)-2-yl)acetamide (2a-d, 3a-f) derivatives using 1,2,4-triazine core along with two
important heterocyles, thiazole and benzothiazole rings.
Method: The acquired ten final compounds were screened to investigate their antitumor activity against
lung adenocarcinoma cell line, A549 and mouse fibroblast cell line, NIH/3T3. Five compounds with higher
antiproliferative activity have been further studied to evaluate whether the cell death due to necrosis or apoptosis
using flow cytometry.
Results and Conclusion: Compound 3b bearing 6-methylbenzothiazole moiety has been established as the most
active antitumor compound with a selective profile and higher apoptotic cell level. All final componds were also
screened against acetylcholine/butyrylcholinesterase enzymes to state their anticholinesterase activity.