Design, Synthesis and Biological Evaluation of Novel 1, 3- thiazolidine-2, 4-diones as Anti-prostate Cancer Agents

Elancheran, R.; Saravanan, K.; Selvaraj, Divakar; Kumari, Sima; Maruthanila, V L; Kabilan, S.; Ramanathan, Muthaiah; Devi, Rajlakshmi; Kotoky, Jibon

doi:10.2174/1871521409666170412121820

Cited by 14 publications

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“…Excessive peroxynitrite radical can be produced by endothelial NO synthase, inducible NO synthase, and neural NO synthase and also produced by the reaction with O 2− , and it might cause many pathological degenerative disorders such as cancer, inflammatory, neurodegenerative, and oxidative damage. [ 12 16 21 22 ] Previous studies have demonstrated that polyphenolic compounds would be the major factor for NO prevention, which might be the reason behind differential inhibitory effects observed in our previous study. [ 2 12 16 17 21 ] In the present study, NO was remarkably inhibited by all the fractions of A. viridis extracts in a dose-dependent manner.…”

Section: Discussionmentioning

confidence: 86%

“…[ 12 16 21 22 ] Previous studies have demonstrated that polyphenolic compounds would be the major factor for NO prevention, which might be the reason behind differential inhibitory effects observed in our previous study. [ 2 12 16 17 21 ] In the present study, NO was remarkably inhibited by all the fractions of A. viridis extracts in a dose-dependent manner. In addition, we further confirm that different fractions of A. viridis showed an excellent metal chelating ability with low IC 50 value.…”

Section: Discussionmentioning

confidence: 94%

“…In addition, the reduction ability of DPPH radicals was determined by the decrease in its absorbance at 517 nm enhanced by different fractions having antioxidant potential. [ 12 21 ] The earlier report also suggested that high polyphenols intake from natural sources such as vegetables and fruits are associated with decreased risk of many degenerative diseases and CVD by attenuated free radicals from the human body. [ 2 12 15 21 ] It was already reported that lower the IC 50 value, the higher is the free radical scavenging capability and vice versa.…”

Section: Discussionmentioning

confidence: 99%

“…[ 12 21 ] The earlier report also suggested that high polyphenols intake from natural sources such as vegetables and fruits are associated with decreased risk of many degenerative diseases and CVD by attenuated free radicals from the human body. [ 2 12 15 21 ] It was already reported that lower the IC 50 value, the higher is the free radical scavenging capability and vice versa. [ 2 12 ] Herein, from this study, it is revealed that MEs of A. viridis have excellent antioxidant potential as compared to AE, CE, and HE, which was quite in similar with the previous reports.…”

Section: Discussionmentioning

confidence: 99%

“…[ 2 12 15 16 21 ] In our previous report, the phenolic compounds of A. viridis revealed significantly minimized Fe3+/ferricyanide complex into the ferrous form (Fe2+); the yellow color of test sample changes to blue and green colors depending on the reducing ability of antioxidant activity. [ 21 ] However, in this study, the reducing capability of the tested different fractions of A. viridis was quite corroborated with earlier studies. [ 2 ] These findings indicated that the A. viridis extract had noticed the difference in ferric ions (Fe3+) reducing power.…”

Section: Discussionmentioning

confidence: 99%

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Phytochemical screening, antioxidant, antityrosinase, and antigenotoxic potential of Amaranthus viridis extract

Kumari

Elancheran

Devi³

2018

Indian J Pharmacol

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OBJECTIVE:Amaranthus viridis (Amaranthaceae) widely distributed all over the world, growing under a wide range of climatic conditions and has been utilized as a medicinal herb in traditional Ayurvedic medicine as antipyretic agents, also for the treatment of inflammation, ulcer, diabetic, asthma and hyperlipidemia. The aim of the study was designed to evaluate the chemical composition and antioxidant and biological properties of different fractions obtained from A. viridis.MATERIALS AND METHODS:Four different extracts of A. viridis were prepared using aqueous, methanol, chloroform, and hexane and investigated their antioxidant potential using free radical scavenging activities such as 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azinobis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS), and nitric oxide (NO) radical scavenging activity, as well as metal chelating activity. In addition, antityrosinase and antigenotoxicity properties were also evaluated by the standard in vitro methods. Finally, the active methanolic extract (ME) was investigated for identifying the phenolic compounds using UPLC-MS/MS.RESULTS:In the present study, chlorogenic acid, gulonic acid, and kaempferol were found to be the major components responsible for the antioxidant activity of A. viridis extract as evidenced from UPLC-MS/MS. Furthermore, the ME of A. viridis revealed excellent antioxidant activities such as DPPH radical scavenging activity (IC50= 47.23 ± 0.66 μg/mL), NO radical scavenging activity (IC50= 64.33 ± 2.01 μg/mL), hydrogen peroxide (H2O2) radical scavenging activity (IC50= 33.21 ± 3.3 μg/mL), ABTS radical scavenging activity (IC50= 47.61 ± 1.31 μg/mL), metal chelating activity (IC50= 32.1 ± 1.11 μg/mL), as well as lipid peroxidation inhibiting activity (IC50= 112 ± 1.21 μg/mL). Furthermore, ME revealed that the protective effects of extract were observed on H2O2-induced DNA damages with alkaline comet assay.CONCLUSIONS:Taken together, the study concluded that the promising antioxidant capacities of A. viridis extract can further be utilized in various agricultural, pharmaceutical, and food applications.

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Section: Discussionmentioning

confidence: 86%

Section: Discussionmentioning

confidence: 94%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Phytochemical screening, antioxidant, antityrosinase, and antigenotoxic potential of Amaranthus viridis extract

Kumari

Elancheran

Devi³

2018

Indian J Pharmacol

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Synthesis, crystal structure investigation and computational approach to discover potential hydrazide derivatives as a potent inhibitor of cyclooxygenase‐2 enzyme

Bakri

Mohamed

Ahmad

et al. 2022

J Biochem & Molecular Tox

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This study reports the synthesis of two new hydrazide derivatives, namely, (E)‐N′‐(4‐ bromobenzylidene)−2‐(4‐isobutylphenyl)propanehydrazide (4a) and (E)‐N′‐benzylidene‐2‐(4‐isobutylphenyl)propanehydrazide (4b), respectively. The compounds were synthesized by the reaction of benzaldehyde with Ibuprofen acid hydrazide. Their structures were confirmed by X‐ray crystallography. To try to do a more detailed investigation, computational studies including Hirshfeld surface analyses, energy frameworks, density functional theory (DFT) optimizations, frontier orbital analyses, molecular electrostatic potential analyses, and natural bond orbital analyses of the studied compounds are performed. Moreover, molecular docking and dynamics simulations of complexes of the compounds with the cyclooxygenase‐2 (COX‐2) enzyme were performed to determine the anti‐inflammatory potential of the compounds. These analyses predicted the compounds to show maximum chemical interactions and be dynamically stable during simulation time. Furthermore, estimation of binding free energies confirmed the high binding affinity of the compounds for the COX‐2 enzyme.

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Green synthesis, Single‐Crystal X‐RD, Hirshfeld Analysis and Anti‐Covid‐19 Molecular Docking Investigation of Symmetrical Azines

Ramkumar

Rajalakshmi

2023

ChemistrySelect

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The 1,2-bis(3,4-dimethoxybenzylidene)hydrazine (VAHD) and 1,2-bis(3-methoxy-4-hydroxybenzylidene)hydrazine (VNHD) are synthesised in a solvent free and catalyst free by greener method (MW). Both the compounds are characterized by FT-IR, 1 H NMR and 13 C NMR spectral studies. Single crystal XRD analysis provides more information on the structure of the compounds VAHD and VNHD. The energy gap (E g ), frontier orbital energies (E HOMO , E LUMO ) and reactivity parameters like chemical hardness and global hardness andMulliken charges are calculated using density functional theory with B3LYP/6-311 + + G(d,p) basis set. The experimental and theoretical calculated IR frequencies and NMR chemical shifts values are compared by DFT method. Hirshfeld surface analysis was conducted to study structure and molecular properties. Molecular docking of symmetrical azine at the active sites of SARS-COVID receptors was investigated. Furthermore, the swissADME online application was used to analyse the physicochemical and pharmacokinetic features of the compounds (VAHD and VNHD).

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Design, Synthesis and Biological Evaluation of Novel 1, 3- thiazolidine-2, 4-diones as Anti-prostate Cancer Agents

Abstract: These findings may provide the essential information for the development of anti-prostate cancer agents.

Cited by 14 publications

References 0 publications

Phytochemical screening, antioxidant, antityrosinase, and antigenotoxic potential of Amaranthus viridis extract

Phytochemical screening, antioxidant, antityrosinase, and antigenotoxic potential of Amaranthus viridis extract

Synthesis, crystal structure investigation and computational approach to discover potential hydrazide derivatives as a potent inhibitor of cyclooxygenase‐2 enzyme

Green synthesis, Single‐Crystal X‐RD, Hirshfeld Analysis and Anti‐Covid‐19 Molecular Docking Investigation of Symmetrical Azines

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