Synthesis and biological evaluation of hydroxyl-substituted Schiff-bases containing ferrocenyl moieties

Chen, Wansong; Ou, Weizhu; Wang, Liqiang; Hao, Yuanqiang; Cheng, Jiashun; Li, Juan; Liu, You‐Nian

doi:10.1039/c3dt51977e

Cited by 63 publications

(26 citation statements)

References 49 publications

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“…Cancer is a broad term to describe a disease that characterized by the uncontrolled proliferation of cells resulting from the disruption or dysfunction of regulatory signaling pathways that Molecular Docking are normally under tight control [20,21]. In modern life, cancer is one of the big health killers.…”

Section: Morpholine Hydrazone Scaffold: Synthesis Anticancer Activitmentioning

confidence: 99%

Molecular Docking Studies of Enzyme Inhibitors and Cytotoxic Chemical Entities

Sultan¹,

Singh²,

Ashraf³

et al. 2018

Molecular Docking

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Docking is a powerful approach to perform virtual screening on large library of compounds, rank the conformations using a scoring function, and propose structural hypotheses of how the ligands inhibit the target, which is invaluable in lead optimization. Using experimentally proven active compounds, detailed docking studies were performed to determine the mechanism of molecular interaction and its binding mode in the active site of the modeled yeast α-glucosidase and human intestinal maltase-glucoamylase. All active ligands were found to have greater binding affinity with the yeast α-glucosidase as compared to that of human homologs, intestinal, and pancreatic maltase, by an average value of~À1.3 and~À0.8 kcal/ mol, respectively. Thirty quinoline derivatives have been synthesized and evaluated against β-glucuronidase inhibitory potential. Twenty-four analogs, which showed outstanding βglucuronidase activity, have IC 50 values ranging between 2.11 AE 0.05 and 46.14 AE 0.95 μM than standard D-saccharic acid 1,4-lactone (IC 50 = 48.4 AE 1.25 μM). Structure activity relationship and the interaction of the active compounds and enzyme active site with the help of docking studies were established. In addition, Small series of morpholine hydrazones synthesized to form morpholine hydrazones scaffold. The in vitro anti-cancer potential of all these compounds were checked against human cancer cell lines such as HepG2 (Human hepatocellular liver carcinoma) and MCF-7 (Human breast adenocarcinoma). Molecular docking studies were also performed to understand the binding interaction.

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Section: Morpholine Hydrazone Scaffold: Synthesis Anticancer Activitmentioning

confidence: 99%

Molecular Docking Studies of Enzyme Inhibitors and Cytotoxic Chemical Entities

Sultan¹,

Singh²,

Ashraf³

et al. 2018

Molecular Docking

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“…Many reports so far on Schiff bases have given rise to several new compounds, and some of them are biologically relevant. The ease with which the Schiff base are designed and prepared have made them to be referred as "fortunate ligands", with C = N linkage which is relevant for antibacterial, antifungal, antioxidant, anticancer, and diuretic activities [8] [9] [10] [11]. Schiff bases with various donor atoms (like N, O, S, etc.)…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Antibacterial Activities of Polydentate Schiff Bases, Based on Salicylaldehyde

Bayeh¹,

Mohammed²,

Gebrezgiabher³

et al. 2020

ABC

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Three Schiff bases L 1 , L 2 and L 3 were synthesized by condensing salicylaldehyde with 4-aminoantipyrine, ethylendiamine and 2-aminophenol respectively and subsequently characterized by various physicochemical investigations.All the three compounds were screened for their In-vitro antibacterial activity against two gram positive bacteria, Staphylococcus aureus (S.A), Staphylococcus epidermidis (S.E) and two gram negative bacteria Klebsiella pneumoniae (K.P) and Pseudomonas aeruginosa (P.A) by agar diffusion method. On comparing the results obtained with the activity of commercially available antibiotics such as Ciprofloxacin and Chloramphenicol, the newly synthesized compounds showed comparable antibacterial activities. The solvent methanol exhibit activity against all bacterial species with IZs ranging from 8 ± 0.25 to 17 ± 0.29 mm while the standard antibiotics Ciprofloxacin and Chloramphenicol exhibited an activities with IZs varying from 21.3 ± 0.31 to 28.3 ± 0.32 and 26.3 ± 0.24 mm to 32.3 ± 0.23 mm, respectively. However, the newly synthesized Schiff bases L 1 , L 2 and L 3 showed IZs ranging from 7.4 ± 0.23 to 32.5 ± 0.14, 3 ± 0.57 to 12 ± 0.28 and 10 ± 0.20 to 32 ± 0.36 respectively. Among the Schiff bases, L 3 showed the activity (32 ± 0.36) against S.E and P.A which is higher than the activity of standard antibiotics Ciprofloxacin and Chloramphenicol against the same bacterial strains. The results obtained revealed that all the synthesized Schiff bases exhibit appreciable antibacterial activity against all the bacteria species which potentially makes them, to apply as wide range antibacterial drugs, after further in-vivo cytotoxicity investigations. Their activity can also be further modified by changing the functionali-

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“…Recently, the hydroxy-substituted Schiff bases have received considerable attention due to good anticancer activity; for example, Luiet al report a new Schiff base (N-(3,4-dihydroxybenzylidene) ferroceneamine, with an excellent biological activity against the HeLa cancer cell line, where the o-dihydroxy groups play an important role. 12,13 Schiff bases have received a considerable amount of attention from many researchers owing to their importance in exhibiting thermochromism and photochromism [14][15][16][17] .Thiourea compounds work as building blocks in the synthesis of heterocyclic compounds. Substituted thioureas have recently gained much interest in the preparation of a wide variety of biologically active compounds 18,19 .…”

Section: Introductionmentioning

confidence: 99%

Novel Synthesis and Characterisation of Some Benzylidene Derivatives of Glycosyl Thiocarbamides

Kadu¹,

Korpe²

2019

RJC

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Several per-O-acetyl and per-O-benzoyl glycosylthiocarbamides were synthesized by the interaction of glycosylisothiocyanates and o-phenylenediamine. While these thiocarbamideson further reactions with anisaldehyde give respective benzylidene derivatives. The identities of these newly synthesized compounds were established on the basis of usual chemical transformations, IR, 1 H NMR, 13 C NMR and Mass spectral studies. All the synthesized compounds have been evaluated for their antibacterial and antifungal activity against different bacteria and fungi by the agar diffusion method.

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Synthesis and biological evaluation of hydroxyl-substituted Schiff-bases containing ferrocenyl moieties

Cited by 63 publications

References 49 publications

Molecular Docking Studies of Enzyme Inhibitors and Cytotoxic Chemical Entities

Molecular Docking Studies of Enzyme Inhibitors and Cytotoxic Chemical Entities

Synthesis, Characterization and Antibacterial Activities of Polydentate Schiff Bases, Based on Salicylaldehyde

Novel Synthesis and Characterisation of Some Benzylidene Derivatives of Glycosyl Thiocarbamides

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