» Articles » PMID: 32837812

Design, Synthesis, and Biological Evaluation of 1,2,4-Thiadiazole-1,2,4-Triazole Derivatives Bearing Amide Functionality As Anticancer Agents

Overview
Journal Arab J Sci Eng
Publisher Springer
Date 2020 Aug 25
PMID 32837812
Citations 7
Authors
Affiliations
Soon will be listed here.
Abstract

A novel library of amide functionality having 1,2,4-thiadiazole-1,2,4-triazole () analogs was designed, synthesized, and structures were characterized by H NMR, C NMR, and mass (ESI-MS) spectral data. Further, all compounds were evaluated for their anticancer activities against four different cancer cell lines including breast cancer (MCF-7, MDA MB-231), lung cancer (A549), and prostate cancer (DU-145) by MTT reduction assay method, and etoposide acts as a standard drug. The results confirmed that majority of the synthesized compounds showed moderate to potent anticancer activities aligned with four cell lines. Among the synthesized compounds, and displayed more potent activity along with inhibitory concentration values ranging from 0.10 ± 0.084 to 11.5 ± 6.49 µM than the standard IC values, which ranges from 1.91 ± 0.84 to 3.08 ± 0.135 µM, respectively.

Citing Articles

Anticancer Activity of Ether Derivatives of Chrysin.

Sokal A, Mruczek P, Niedoba M, Dewalska A, Stocerz K, Kadela-Tomanek M Molecules. 2025; 30(4).

PMID: 40005270 PMC: 11857933. DOI: 10.3390/molecules30040960.


Discovery of Novel and Selective Schiff Base Inhibitors as a Key for Drug Synthesis, Molecular Docking, and Pharmacological Evaluation.

Khan I, Rehman W, Rasheed L, Rahim F, Hussain R, Khan S ACS Omega. 2024; 9(28):31148-31158.

PMID: 39035878 PMC: 11256303. DOI: 10.1021/acsomega.4c04599.


evaluation on potential inhibitors data: DFT and molecular modelling approaches.

Oyebamiji A, Akintelu S, Adekunle D, Oke D, Olanrewaju A, Akinola O Data Brief. 2024; 55:110565.

PMID: 38952955 PMC: 11214998. DOI: 10.1016/j.dib.2024.110565.


Synthesis, Anticancer Activity, and In Silico Studies of 5-(3-Bromophenyl)--aryl-4-1,2,4-triazol-3-amine Analogs.

Ahsan M, Gautam K, Ali A, Ali A, Altamimi A, Salahuddin Molecules. 2023; 28(19).

PMID: 37836779 PMC: 10574406. DOI: 10.3390/molecules28196936.


Design, synthesis and evaluation of novel 1,2,4-triazole derivatives as promising anticancer agents.

Emami L, Sadeghian S, Mojaddami A, Khabnadideh S, Sakhteman A, Sadeghpour H BMC Chem. 2022; 16(1):91.

PMID: 36369166 PMC: 9652805. DOI: 10.1186/s13065-022-00887-x.


References
1.
Porta C, Riboldi E, Sica A . Mechanisms linking pathogens-associated inflammation and cancer. Cancer Lett. 2010; 305(2):250-62. DOI: 10.1016/j.canlet.2010.10.012. View

2.
Asami T, Min Y, Nagata N, Yamagishi K, Takatsuto S, Fujioka S . Characterization of brassinazole, a triazole-type brassinosteroid biosynthesis inhibitor. Plant Physiol. 2000; 123(1):93-100. PMC: 58985. DOI: 10.1104/pp.123.1.93. View

3.
Leung-Toung R, Wodzinska J, Li W, Lowrie J, Kukreja R, Desilets D . 1,2,4-thiadiazole: a novel Cathepsin B inhibitor. Bioorg Med Chem. 2003; 11(24):5529-37. DOI: 10.1016/j.bmc.2003.09.040. View

4.
Khan F, Akhtar S, Sheikh M . Cancer treatment - objectives and quality of life issues. Malays J Med Sci. 2012; 12(1):3-5. PMC: 3349406. View

5.
Kumar D, Kumar N, Chang K, Gupta R, Shah K . Synthesis and in-vitro anticancer activity of 3,5-bis(indolyl)-1,2,4-thiadiazoles. Bioorg Med Chem Lett. 2011; 21(19):5897-900. DOI: 10.1016/j.bmcl.2011.07.089. View