Synthesis and biological assessment of ciprofloxacin-derived 1,3,4-thiadiazoles as anticancer agents

Ahadi, Hamideh; Shokrzadeh, Mohammad; Hosseini‐Khah, Zahra; Ghassemi-Barghi, Nasrin; Ghasemian, Majid; Emadi, Elnaz; Zargari, Mehryar; Razzaghi‐Asl, Nima; Emami, Saeed

doi:10.1016/j.bioorg.2020.104383

Cited by 27 publications

(14 citation statements)

References 25 publications

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“…The fluorine atom boosts penetration into bacterial cells and improves the antibacterial activity to 30 times higher than that of quinolones. Furthermore, the 5-fluoroisatin moiety improves the lipophilicity of drugs while increasing the antimycobacterial activity [ 10 ]. Substituents at C-7 can directly interact with DNA helicase or topoisomerase IV, and nitrogen-containing five- or six-atom alkaline heterocycles, such as piperazine, exhibit good activity.…”

Section: Dna Topoisomerase Inhibitorsmentioning

confidence: 99%

A Comprehensive Overview of the Antibiotics Approved in the Last Two Decades: Retrospects and Prospects

et al. 2023

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Due to the overuse of antibiotics, bacterial resistance has markedly increased to become a global problem and a major threat to human health. Fortunately, in recent years, various new antibiotics have been developed through both improvements to traditional antibiotics and the discovery of antibiotics with novel mechanisms with the aim of addressing the decrease in the efficacy of traditional antibiotics. This manuscript reviews the antibiotics that have been approved for marketing in the last 20 years with an emphasis on the antibacterial properties, mechanisms, structure–activity relationships (SARs), and clinical safety of these antibiotics. Furthermore, the current deficiencies, opportunities for improvement, and prospects of antibiotics are thoroughly discussed to provide new insights for the design and development of safer and more potent antibiotics.

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Section: Dna Topoisomerase Inhibitorsmentioning

confidence: 99%

A Comprehensive Overview of the Antibiotics Approved in the Last Two Decades: Retrospects and Prospects

et al. 2023

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“…Wound tissue was collected and tissue homogenates were prepared for the measurement of lipid peroxidation rate by measuring the level of malondialdehyde (MDA) using the TBA reaction by method of Uchiyama and Mihara [39,40].…”

Section: Determination Of Lipid Peroxidationmentioning

confidence: 99%

An in vivo investigation on the wound-healing activity of Specific ligand for the innate repair receptor, ARA290, using a diabetic animal model

Mashreghi¹,

Bayrami

Sichani

et al. 2023

Preprint

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The diabetic foot ulcer (DFU) are serious problems to diabetes and may be associated with late healing and septic manifestation, consequently result in amputation which is an extortionate incident. The innate repair receptor (IRR) is expressed by injured tissues and is activated by erythropoietin produced and released into damaged tissue. Activation of the IRR might provide benefit for diabetic wound healing. This study evaluated effect of a specific IRR agonist, ARA290, on skin wound repair. The aim of the present study was to evaluate the effect of topical application based on ARA290, in streptozotocin-induced diabetic incision wound models rats. The treatment was performed daily, until day 14 after wound induction. Wound closure was determined and the features of the repaired tissue were examined, including amount of collagen and protein content, biochemical parameters, antioxidant status and proinflammatory cytokines. The data confirmed wound healing activities via macroscopic, biochemical, immunofluorescent and molecular methods. There was meaningful acceleration in wound closure rate, decrease in the period of re-epitalization, greater amount of collagen and protein content in ARA290 treated group when compared with control group. The increase of serum insulin and HDL was divergent with blood glucose decrease and reduced lipid level. The healing effect was confirmed by reduced levels of inflammatory cytokines and lipid peroxidation and augmented antioxidants. The results propose that ARA290-arbitrated IRR activation may signify an appealing approach to treat diabetes-associated wound healing.

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“…Penta-heterocycles framework is an exceptionally adaptable drug-like format that is being utilised broadly in the structure of cancer treatments and cellular apoptosis such as pyrazoles, which were reported in a variety of potent anti-cancer active agents as listed on Ruxolitinib 16 and Compound A 17 ( Figure 1 ). Furthermore, 1,3,4-thiadiazoles such as Compound B 18 was reported as highly anti-cancer agent by inducing apoptosis significantly in MCF-7 cell ( Figure 1 ). Substituted 1,2,4-triazazole (Compound C ) 19 also displayed remarkable epidermal growth factor receptor (EGFR) inhibition activity with IC 50 value of 19.8 nM ( Figure 1 ).…”

Section: Introductionmentioning

confidence: 99%

Synthesis and biological assessment of indole derivatives containing penta-heterocycles scaffold as novel anticancer agents towards A549 and K562 cells

Zhang

Tang

Fan

et al. 2023

Journal of Enzyme Inhibition and Medicinal Chemistry

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Herein, a new series of 2-chloro- N -(5-(2-oxoindolin-3-yl)-4 H -pyrazol-3-yl) acetamide derivatives containing 1,3,4 - thiadiazole ( 10a – i ) and 4 H -1,2,4-triazol-4-amine ( 11a – r ) moiety was designed, synthesised as novel anticancer agents. The antiproliferative activity values indicated that compound 10 b stood as the most potent derivative with IC 50 values of 12.0 nM and 10 nM against A549 and K562 cells, respectively. Mechanism investigation and docking studies of 10 b indicated that it possessed good apoptosis characteristic and dose-dependent growth arrest of A549 and K562 cells, blocked cell cycle into G2/M phase. Interestingly, 10 b suppressed the growth of A549 and K562 cells via modulation of EGFR and p53-MDM2 mediated pathway.

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Synthesis and biological assessment of ciprofloxacin-derived 1,3,4-thiadiazoles as anticancer agents

Cited by 27 publications

References 25 publications

A Comprehensive Overview of the Antibiotics Approved in the Last Two Decades: Retrospects and Prospects

A Comprehensive Overview of the Antibiotics Approved in the Last Two Decades: Retrospects and Prospects

An in vivo investigation on the wound-healing activity of Specific ligand for the innate repair receptor, ARA290, using a diabetic animal model

Synthesis and biological assessment of indole derivatives containing penta-heterocycles scaffold as novel anticancer agents towards A549 and K562 cells

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