Biological Activity Evaluation of Novel 1,2,4-Triazine Derivatives Containing Thiazole/Benzothiazole Rings.
Anticancer Agents Med Chem
; 17(13): 1846-1853, 2017.
Article
in En
| MEDLINE
| ID: mdl-28356019
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 ANDCONCLUSION:
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.Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Thiazoles
/
Triazines
/
Benzothiazoles
/
Antineoplastic Agents
Limits:
Animals
/
Humans
Language:
En
Journal:
Anticancer Agents Med Chem
Journal subject:
ANTINEOPLASICOS
/
QUIMICA
Year:
2017
Document type:
Article