title: Biological Activity Evaluation of Novel 1,2,4-Triazine Derivatives Containing Thiazole/Benzothiazole Rings.
abstract: Triazine ring is a prominent structural motif found in some azanucleosides whose efficiency improved many times in the research area of antitumor agents.
  
  
  
  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.
  
  
  
  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.
  
  
  
  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.
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University, 26470 Eskisehir. Turkey.
authors.forename: Leyla
authors.initials: L
authors.lastname: Yurttas
authors.affiliation: Faculty of Pharmacy, Department of Biohemistry, Anadolu University, 26470 Eskisehir. Turkey.
authors.forename: Gulsen Akalin
authors.initials: GA
authors.lastname: Ciftci
authors.affiliation: Faculty of Pharmacy, Department of Biohemistry, Anadolu University, 26470 Eskisehir. Turkey.
authors.forename: Halide Edip
authors.initials: HE
authors.lastname: Temel
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University, 26470 Eskisehir. Turkey.
authors.forename: Begum Nurpelin
authors.initials: BN
authors.lastname: Saglik
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University, 26470 Eskisehir. Turkey.
authors.forename: Bahar
authors.initials: B
authors.lastname: Demir
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University, 26470 Eskisehir. Turkey.
authors.forename: Serkan
authors.initials: S
authors.lastname: Levent
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D052160:Benzothiazoles / Q000737:chemistry*; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D061986:MCF-7 Cells; D051379:Mice; D041681:NIH 3T3 Cells; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry*; D014227:Triazines / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D052160:Benzothiazoles; D013844:Thiazoles; D014227:Triazines; C093444:1,2,4-triazine; C005465:benzothiazole
keywords: Triazine; antiproliferative activity; apoptosis; benzothiazole; lung cancer; thiazole