Recent updates on 1,2,3-triazole-containing hybrids with in vivo therapeutic potential against cancers: A mini-review

European Journal of Medicinal Chemistry, Год журнала: 2023, Номер 251, С. 115254 - 115254

Опубликована: Март 6, 2023

Язык: Английский

---

Recent advances in 1,2,3- and 1,2,4-triazole hybrids as antimicrobials and their SAR: A critical review

European Journal of Medicinal Chemistry, Год журнала: 2023, Номер 259, С. 115603 - 115603

Опубликована: Июль 16, 2023

Язык: Английский

---

Identification of new benzimidazole-triazole hybrids as anticancer agents: multi-target recognition, in vitro and in silico studies

Journal of Enzyme Inhibition and Medicinal Chemistry, Год журнала: 2023, Номер 38(1)

Опубликована: Янв. 18, 2023

Multi-target inhibitors represent useful anticancer agents with superior therapeutic attributes. Here in, two novel series of benzimidazole-triazole hybrids were designed, synthesised as multi-target EGFR, VEGFR-2 and Topo II inhibitors, evaluated for activity. Compounds 5a 6g the most potent analogues against four cancer cell lines, HepG-2, HCT-116, MCF-7 HeLa, further VEGFR-2, inhibition. Compound was especially good inhibitor EGFR (IC50 = 0.086 µM) compared to Gefitinib 0.052 µM), moderate 0.107 Sorafenib 0.0482 stronger 2.52 than Doxorubicin 3.62 µM). exhibited inhibition weaker DNA binding assay, cycle analysis, apoptotic induction, molecular docking, physicochemical studies additionally implemented explore plausible mechanism active compounds.

Язык: Английский

---

The fate of heterogeneous catalysis & click chemistry for 1,2,3-triazoles: Nobel prize in chemistry 2022

Catalysis Communications, Год журнала: 2023, Номер 176, С. 106629 - 106629

Опубликована: Фев. 23, 2023

The demand for environmental friendly methodologies had shifted the approach of scientific community using easy and green reaction conditions instead hazardous harsh conditions. One suggested approaches, use catalyst remained prime choice free reaction. difficulty in separation homogeneous from product increased attention chemists heterogeneous catalysts. present review summarizes some recent important developments catalysis "click reaction" obtaining 1,2,3-triazoles via Cu-catalyzed 1,3-dipolar azide-alkyne cycloaddition (CuAAC). A vast collection papers is efficiently grouped into two significant classes to increase readability language. Firstly, CuAAC reactions, secondly, other metal-catalyzed (MAAC) reactions are discussed. further sub-classes Cu(I)-nanoparticle catalyzed (Cu-NPs-AAC) simple Cu(I)-catalyzed (CuAAC) reactions. In most cases, formation 1,4-disubstituted 1,2,3-triazoles, as reported, was conveniently presented with help colored schemes.

Язык: Английский

---

Innovation of some novel complexes based on 1‐(4‐nitrophenyl)‐1H‐1,2,3‐triazol‐4‐yl)methanol ligand: Synthesis, structural elucidation DFT calculation and pharmaceutical studies

Applied Organometallic Chemistry, Год журнала: 2024, Номер 38(6)

Опубликована: Апрель 25, 2024

Novel divalent chelates of Co (II), Cu Zn (II) and Ni were prepared described the form [M (NTM)(CH 3 COO) 2 ] where NTM = [1‐(4‐nitrophenyl)‐1H‐1,2,3‐triazol‐4‐yl)methanol ligand. Elemental analyses, infrared red, 1 H 13 CNMR, electronic, magnetic susceptibility, conductivity measurements X‐ray diffraction studies used to assess our metal complexes. Moreover, stability stoichiometry novel examined through job's method in solutions. Correlation all spectroscopic techniques states that acts as a bi‐dentate NO ligand afford octahedral complex geometry for investigated chelates. Thermodynamic kinetics factors various thermal degradation phases calculated. B3LYP/LANL2DZ/6‐311 g(d,p) theoretical study has been applied estimating MEP quantum chemical reactivity descriptors studied molecules. UV–Vis absorption spectra molecules are predicted via time‐dependent DFT (TD‐DFT) calculations. In addition, MOE‐ docking was tested on two different proteins, receptor (3HB5) breast cancer mutant oxidoreductase well Glucosamine‐6‐phosphate synthase with glucosamine‐6‐ phosphate (2VF5) E.coli COVID‐19 protease. The results recommended (NTMCo), (NTMNi), (NTMCu) (NTMZn) complexes showed highest inhibitory activity compared other ligands antimicrobial candidates. Furthermore, in‐vitro anti‐bacterial, anti‐fungal, cytotoxic anti‐oxidant performances selected its studied. All presented superiority, proceeding free organic ineffective management, definitely NTMCu complex.

Язык: Английский

---

Emerging impact of triazoles as anti-tubercular agent

European Journal of Medicinal Chemistry, Год журнала: 2022, Номер 238, С. 114454 - 114454

Опубликована: Май 13, 2022

Язык: Английский

---

The 1,2,3-triazole ‘all-in-one’ ring system in drug discovery: a good bioisostere, a good pharmacophore, a good linker, and a versatile synthetic tool

Expert Opinion on Drug Discovery, Год журнала: 2022, Номер 17(11), С. 1209 - 1236

Опубликована: Сен. 27, 2022

The 1,2,3-triazole ring occupies an important space in medicinal chemistry due to its unique structural properties, synthetic versatility and pharmacological potential making it a critical scaffold. Since is readily available through click for creating compound collections against various diseases, has become emerging area of interest chemists.This review article addresses the properties the1,2,3-triazole nucleus as intriguing system drug discovery while focusing on most recent strategies exploited design development analogs inhibitors biological targets.Evidently, with features enormous diseases pharmacophore, bioisoster or platform. evidence indicates that may be more molecules near future along increasing understanding prominent roles structures. feasibility triazole make certainly ideal libraries constructive structure-activity relationship studies. However, comparative target-specific studies are needed gain deeper molecular recognition.[Figure: see text].

Язык: Английский

---

Structure–Activity Relationship of Benzofuran Derivatives with Potential Anticancer Activity

Cancers, Год журнала: 2022, Номер 14(9), С. 2196 - 2196

Опубликована: Апрель 28, 2022

Benzofuran is a heterocyclic compound found naturally in plants and it can also be obtained through synthetic reactions. Multiple physicochemical characteristics versatile features distinguish benzofuran, its chemical structure composed of fused benzene furan rings. derivatives are essential compounds that hold vital biological activities to design novel therapies with enhanced efficacy compared conventional treatments. Therefore, medicinal chemists used core synthesize new applied variety disorders. exhibited potential effectiveness chronic diseases such as hypertension, neurodegenerative oxidative conditions, dyslipidemia. In acute infections, benzofuran revealed anti-infective properties against microorganisms like viruses, bacteria, parasites. recent years, the complex nature number acquired or resistant cancer cases have been largely increasing. anticancer activity lower incidence severity adverse events normally encountered during chemotherapeutic This review discusses structure–activity relationship (SAR) several order elucidate possible substitution alternatives structural requirements for highly potent selective activity.

Язык: Английский

---

New 1,2,3-triazole linked ciprofloxacin-chalcones induce DNA damage by inhibiting human topoisomerase I& II and tubulin polymerization

Journal of Enzyme Inhibition and Medicinal Chemistry, Год журнала: 2022, Номер 37(1), С. 1346 - 1363

Опубликована: Май 11, 2022

A series of novel 1,2,3-triazole-linked ciprofloxacin-chalcones 4a-j were synthesised as potential anticancer agents. Hybrids exhibited remarkable anti-proliferative activity against colon cancer cells. Compounds displayed IC50s ranged from 2.53-8.67 µM, 8.67-62.47 and 4.19-24.37 µM for HCT116, HT29, Caco-2 cells; respectively, whereas the doxorubicin, showed IC50 values 1.22, 0.88, 4.15 µM. 4a, 4b, 4e, 4i, 4j most potent HCT116 with 3.57, 4.81, 4.32, 4.87, 2.53 compared to doxorubicin (IC50 = 1.22 µM). Also, hybrids inhibitory activities topoisomerase I, II, tubulin polymerisation. They increased protein expression level γH2AX, indicating DNA damage, arrested in G2/M phase, possibly through ATR/CHK1/Cdc25C pathway. Thus, ciprofloxacin could be exploited leads further investigation medicines fight colorectal carcinoma.

Язык: Английский

---

Current development of 1,2,3-triazole derived potential antimalarial scaffolds: Structure- activity relationship (SAR) and bioactive compounds

European Journal of Medicinal Chemistry, Год журнала: 2023, Номер 259, С. 115699 - 115699

Опубликована: Июль 30, 2023

Язык: Английский

---