Design, Synthesis, Cytotoxicity Evaluation and Docking Studies of 1,2,4-Triazine Derivatives Bearing Different Arylidene-Hydrazinyl Moieties As Potential Mtor Inhibitors

Design, Synthesis, Cytotoxicity Evaluation and Docking Studies of 1,2,4-Triazine Derivatives Bearing Different Arylidene-Hydrazinyl Moieties As Potential Mtor Inhibitors Publisher

Ranjbar S^{1, 2} ; Edraki N² ; Khoshneviszadeh M² ; Foroumadi A³ ; Miri R² ; Khoshneviszadeh M²

Show Affiliations

1. Department of Medicinal Chemistry, School of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran
2. Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
3. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

Source: Research in Pharmaceutical Sciences Published:2018

Abstract

Mammalian target of rapamycin (mTOR) is a phosphoinositide 3-kinase-related protein kinase which controls cell growth and is frequently deregulated in many cancers. Therefore, mTOR inhibitors are used as antineoplastic agents for cancer treatment. In this study, 1,2,4-triazine derivatives containing different arylidene-hydrazinyl moieties were designed and synthesized. Cytotoxicity of the compounds was evaluated on HL-60 and MCF-7 cell lines by MTT assay. S1, S2 and S3 exhibited good cytotoxic activity on both cell lines with an IC50 range of 6.42 - 20.20 μM. In general, substitution of a five-membered heterocyclic ring containing NO2, such as 5-nitrofuran-2-yl, resulted in the best potency. Molecular docking analysis was performed to study the possible interactions and binding modes of all the triazine derivatives with mTOR receptor. The most promising compound, S1, was well accommodated within the active site and had the least estimated free energy of binding (even less than the inherent ligand of the protein, PDB ID: 4JT6). It is concluded from both MTT assay and docking studies that the arylidene moiety linked to the hydrazinyl part of the structure had a prominent role in cytotoxicity and mTOR inhibitory activity.

2. Diphenyl-Substituted Triazine Derivatives: Synthesis, Α-Glucosidase Inhibitory Activity, Kinetics and in Silico Studies, Future Medicinal Chemistry (2023)

Experts (# of related papers)

Mohammad Ali Faramarzi (1)

Mohammad Mahdavi (1)

Style	Citing Format
MLA	Ranjbar S, et al.. "Design, Synthesis, Cytotoxicity Evaluation and Docking Studies of 1,2,4-Triazine Derivatives Bearing Different Arylidene-Hydrazinyl Moieties As Potential Mtor Inhibitors." Research in Pharmaceutical Sciences, vol. 13, no. 1, 2018, pp. 1-11.
APA	Ranjbar S, Edraki N, Khoshneviszadeh M, Foroumadi A, Miri R, Khoshneviszadeh M (2018). Design, Synthesis, Cytotoxicity Evaluation and Docking Studies of 1,2,4-Triazine Derivatives Bearing Different Arylidene-Hydrazinyl Moieties As Potential Mtor Inhibitors. Research in Pharmaceutical Sciences, 13(1), 1-11.
Chicago	Ranjbar S, Edraki N, Khoshneviszadeh M, Foroumadi A, Miri R, Khoshneviszadeh M. "Design, Synthesis, Cytotoxicity Evaluation and Docking Studies of 1,2,4-Triazine Derivatives Bearing Different Arylidene-Hydrazinyl Moieties As Potential Mtor Inhibitors." Research in Pharmaceutical Sciences 13, no. 1 (2018): 1-11.
Harvard	Ranjbar S et al. (2018) 'Design, Synthesis, Cytotoxicity Evaluation and Docking Studies of 1,2,4-Triazine Derivatives Bearing Different Arylidene-Hydrazinyl Moieties As Potential Mtor Inhibitors', Research in Pharmaceutical Sciences, 13(1), pp. 1-11.
Vancouver	Ranjbar S, Edraki N, Khoshneviszadeh M, Foroumadi A, Miri R, Khoshneviszadeh M. Design, Synthesis, Cytotoxicity Evaluation and Docking Studies of 1,2,4-Triazine Derivatives Bearing Different Arylidene-Hydrazinyl Moieties As Potential Mtor Inhibitors. Research in Pharmaceutical Sciences. 2018;13(1):1-11.
BibTex	@article{ author = {Ranjbar S and Edraki N and Khoshneviszadeh M and Foroumadi A and Miri R and Khoshneviszadeh M}, title = {Design, Synthesis, Cytotoxicity Evaluation and Docking Studies of 1,2,4-Triazine Derivatives Bearing Different Arylidene-Hydrazinyl Moieties As Potential Mtor Inhibitors}, journal = {Research in Pharmaceutical Sciences}, volume = {13}, number = {1}, pages = {1-11}, year = {2018} }
RIS	TY - JOUR AU - Ranjbar S AU - Edraki N AU - Khoshneviszadeh M AU - Foroumadi A AU - Miri R AU - Khoshneviszadeh M TI - Design, Synthesis, Cytotoxicity Evaluation and Docking Studies of 1,2,4-Triazine Derivatives Bearing Different Arylidene-Hydrazinyl Moieties As Potential Mtor Inhibitors JO - Research in Pharmaceutical Sciences VL - 13 IS - 1 SP - 1 EP - 11 PY - 2018 ER -

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