77164-80-8Relevant academic research and scientific papers
Synthesis, anti-proliferative evaluation, and molecular docking studies of 3-(Alkylthio)-5,6-diaryl-1,2,4-triazines as tubulin polymerization inhibitors
Saravani, Farhad,Moghadam, Ebrahim Saeedian,Salehabadi, Hafezeh,Ostad, Seyednasser,Hamedani, Morteza Pirali,Amanlou, Massoud,Faramarzi, Mohammad Ali,Amini, Mohsen
, p. 1194 - 1201 (2019/11/22)
Background: The role of microtubules in cell division and signaling, intercellular transport, and mitosis has been well known. Hence, they have been targeted for several anti-cancer drugs. Methods: A series of 3-(alkylthio)-5,6-diphenyl-1,2,4-triazines were prepared and evaluated for their cytotoxic activities in vitro against three human cancer cell lines; human colon carcinoma cells HT-29, human breast adenocarcinoma cell line MCF-7, human Caucasian gastric adenocarcinoma cell line AGS as well as fibroblast cell line NIH-3T3 by MTT assay. Docking simulation was performed to insert these compounds into the crystal structure of tubulin at the colchicine binding site to determine a probable binding model. Compound 5d as the most active compound was selected for studying of microtubule disruption. Results: Compound 5d showed potent cytotoxic activity against all cell lines. The molecular modeling study revealed that some derivatives of triazine strongly bind to colchicine binding site. The tubulin polymerization assay kit showed that the cytotoxic activity of 5d may be related to inhibition of tubulin polymerization. Conclusion: The cytotoxicity and molecular modeling study of the synthesized compounds with their inhibition activity in tubulin polymerization demonstrate the potential of triazine derivatives for development of new anti-cancer agents.
Synthesis of unsymmetric 6,6-diaryl-2,2-bipyridines using a 1,2,4-triazine methodology
Kopchuk,Chepchugov,Kim,Zyryanov,Kovalev,Rusinov,Chupakhin
, p. 695 - 698 (2015/11/27)
New unsymmetric 6,6-diaryl-2,2-bipyridines were synthesized in high yields using a "1,2,4-triazine" methodology. Their photophysical properties were studied.
Synthesis and in vitro evaluation of novel 1,2,4-triazine derivatives as neuroprotective agents
Irannejad, Hamid,Amini, Mohsen,Khodagholi, Fariba,Ansari, Niloufar,Tusi, Solaleh Khoramian,Sharifzadeh, Mohammad,Shafiee, Abbas
experimental part, p. 4224 - 4230 (2010/09/12)
The role of novel triazine derivatives against oxidative stress exerted by hydrogen peroxide on differentiated rat pheochromocytoma (PC12) cell line was examined and a consistent protection from H2O2-induced cell death, associated with a marked reduction in caspase-3 activation, was observed. Moreover, activation of NF-κB, a known regulator of a host of genes that involves in specific stress and inflammatory responses by H2O2, was greatly impaired by triazine pretreatment in differentiated PC12 cells. Neuroprotective effect of such compounds may represent a promising approach for treatment of neurodegenerative diseases.
