Design, synthesis and biological evaluation of novel 5-(4-chlorophenyl)-4-phenyl-4H-1,2,4-triazole-3-thiols as an anticancer agent

Patel, Hitesh; Brahmbhatt, Jpan; Pandya, Pranav A.; Daraji, Drashti G.; Rawal, Rakesh; Baran, Sujit K.

doi:10.1016/j.molstruc.2021.130000

Cited by 20 publications

(11 citation statements)

References 29 publications

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“…Based on results obtained from different derivatives, a structure‐activity relationship was also established. In vitro results were further validated by molecular docking experiments and found significant similarity to support the data [73] …”

Section: Synthesis and Biological Evaluation Of Isolated/functionaliz...mentioning

confidence: 64%

“…In vitro results were further validated by molecular docking experiments and found significant similarity to support the data. [73] In several solid tumors, thymidine phosphorylase is over expressed; hence most of the researchers are working on this target to find new lead for cancer treatment. Sohail et al synthesized novel 1,2,4-triazole 50 and derivatives from mercapto-1,2,4-triazoles and chloro or bromo substituted acetic acid at room temperature affording the corresponding product with excellent yield as shown in Scheme 40.…”

Section: Triazole Fused With Phthalazinementioning

confidence: 99%

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Synthetic and Medicinal Perspective of 1,2,4‐Triazole as Anticancer Agents

Rathod

Kumar

2022

Chemistry & Biodiversity

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Cancer is still one of the leading causes of death worldwide. Many researchers are working to design and develop heterocyclic-based drugs with the potential to treat cancer at various stages. There is always an unmet need to discover new anticancer drugs to treat different types of cancer. Based on literature reports, it was evident that hybrid 1,2,4-triazoles exhibit a wide spectrum of biological potential (particularly potent anticancer activity), as compared to the corresponding monocyclic compounds. In this review, we summarized fused/hybrid 1,2,4-triazole and poly-functionalized 1,2,4-triazoles as anticancer agents. Triazole may be fused with other heterocyclic scaffolds like pyrimidine, pyridine, piperidine, quinoxaline, quinazoline, thiadiazine, indole, phthalazine etc. A clear explanation of the method of synthesis, structure-activity relationship, and in vitro results plus the inhibitory concentration of new molecules are focused on in this review article.

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Section: Synthesis and Biological Evaluation Of Isolated/functionaliz...mentioning

confidence: 64%

Section: Triazole Fused With Phthalazinementioning

confidence: 99%

Synthetic and Medicinal Perspective of 1,2,4‐Triazole as Anticancer Agents

Rathod

Kumar

2022

Chemistry & Biodiversity

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“…These derivatives have found applications in various elds, such as medicine and agriculture. For instance, compounds like uconazole and bromuconazole have been utilized as commercial antifungicides [12], while vorozole and anastrozole have been introduced as anticancer medications [13].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization, and Evaluation of Antibacterial and Anticorrosion Properties of 4-Azo-3,5-sustituted-1,2,4-Triazole Polymers

Hamzah,

Mhaibes

2024

Preprint

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In this study, a series of 4-azo derivatives of 1,2,4-triazole were synthesized through the reaction of melt thiocarbohydrazide with various substituted benzoic acids. Subsequently, these derivatives were coupled with different aromatic amines to obtain 4-azo derivatives of 1,2,4-triazole. The synthesized derivatives were then converted into 4-azo-3,5-substituted-1,2,4-triazole polymers using dry acetonitrile, pyridine, and poly acryloyl chloride. The physical properties, FT-IR spectra, and 1H-NMR spectra (for selected compounds) were utilized to confirm the structures of the synthesized compounds and polymers. Furthermore, the antibacterial and anticorrosion activities of the compounds and polymers were investigated.

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“…The electronic properties of nitrogen or sulfur heteroatoms are a significant factor in their selection. One of these compounds, 1,2,4-triazole, has demonstrated a wide range of biological activities such as antibacterial, [5][6][7] antimicrobial, [8][9][10] anti-HIV, [11][12][13] antiviral, [14,15] antitumor, [14][15][16] and antitubercular. [17][18][19][20] Researchers have found that modifying the structure of the triazole moiety with specific molecular groups can enhance its biological potency.…”

Section: Introductionmentioning

confidence: 99%

Novel Antitubercular Agents: Design, Synthesis, Molecular Dynamic and Biological Studies of Pyrazole – 1,2,4‐Triazole Conjugates

Ajin,

Arun Kumar,

Singh

et al. 2023

Chemistry & Biodiversity

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Mycobacterium tuberculosis (Mtb) has numerous cell wall and non‐cell wall mediated receptors for drug action, of which cell wall mediated targets were found to be more promising because of their pivotal role in bacterial protection and survival. Herein, we reported the design and synthesis of a series of pyrazole‐linked triazoles based on the reported structural features of promising drug candidates that target DprE1 receptors through a Structure‐based drug design (SBDD) approach (6a–6j and 7a–7j). The synthesized compounds were evaluated for their in‐vitro antitubercular activity against virulent strains of Mtb H37Rv. In‐silico studies revealed that most compounds exhibit binding interactions with crucial amino acids like Lys418, Tyr314, Tyr60, and Asp386 at DprE1. Furthermore, the protein‐ligand (7j) shows appreciable stability compared to innate protein in a 100 ns molecular dynamic simulation study. In‐vitro MAB assay revealed that 14 compounds exhibit significant antitubercular activity with minimum inhibitory concentration (MIC) of the 3.15–4.87 μM of the 20 compounds tested. An in‐vitro cytotoxicity study on normal cell lines (MCF10) revealed safe compounds (IC50 values:341.85 to 726.08 μM). Hence, the present study opens the development of new pyrazole‐linked triazoles as probable DprE1 inhibitors.

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Design, synthesis and biological evaluation of novel 5-(4-chlorophenyl)-4-phenyl-4H-1,2,4-triazole-3-thiols as an anticancer agent

Cited by 20 publications

References 29 publications

Synthetic and Medicinal Perspective of 1,2,4‐Triazole as Anticancer Agents

Synthetic and Medicinal Perspective of 1,2,4‐Triazole as Anticancer Agents

Synthesis, Characterization, and Evaluation of Antibacterial and Anticorrosion Properties of 4-Azo-3,5-sustituted-1,2,4-Triazole Polymers

Novel Antitubercular Agents: Design, Synthesis, Molecular Dynamic and Biological Studies of Pyrazole – 1,2,4‐Triazole Conjugates

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