Biological Activity Evaluation of Novel 1,2,4-Triazine Derivatives Containing Thiazole/Benzothiazole Rings

Title:Biological Activity Evaluation of Novel 1,2,4-Triazine Derivatives Containing Thiazole/Benzothiazole Rings

Volume: 17 Issue: 13

Author(s): Leyla Yurttas*, Gulsen Akalin Ciftci, Halide Edip Temel, Begum Nurpelin Saglik, Bahar Demir and Serkan Levent

Affiliation:

• Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University, 26470 Eskisehir,Turkey

Keywords: Triazine, thiazole, benzothiazole, antiproliferative activity, lung cancer, apoptosis.

Abstract: 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.

Cite this article as:

Yurttas Leyla*, Ciftci Akalin Gulsen, Temel Edip Halide , Saglik Nurpelin Begum, Demir Bahar and Levent Serkan , Biological Activity Evaluation of Novel 1,2,4-Triazine Derivatives Containing Thiazole/Benzothiazole Rings, Anti-Cancer Agents in Medicinal Chemistry 2017; 17 (13) . https://dx.doi.org/10.2174/1871520617666170327151031