Synthesis, NMR, anti-oxidant, anti-cancer activity, Molecular docking, DFT Calculations and in silico ADME analysis of 3′-benzoyl-4′-phenyl-5′-(piperazin-1-ylmethyl)spiro[indoline-3,2′-pyrrolidin]-2-one derivatives

Rajaraman, D.; Anthony, L. Athishu; Sundararajan, G.; Shanmugam, Maheswaran; Arunkumar, A.

doi:10.1016/j.molstruc.2022.133551

Cited by 9 publications

(3 citation statements)

References 33 publications

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“…The chiral configuration of pyrrolidine ring was not identified and reported by the authors. Some of the synthesized agents revealed considerable antiproliferative properties (MTT assay) against KB cell line (the most potent is the compound with R = Me, IC 50 = 6.5 μM) [ 47 ].…”

Section: Synthetic Spirooxindolesmentioning

confidence: 99%

Spirooxindole: A Versatile Biologically Active Heterocyclic Scaffold

et al. 2023

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Spirooxindoles occupy an important place in heterocyclic chemistry. Many natural spirooxindole-containing compounds have been identified as bio-promising agents. Synthetic analogs have also been synthesized utilizing different pathways. The present article summarizes the recent development of both natural and synthetic spirooxindole-containing compounds prepared from isatin or its derivatives reported in the last five years. The spirooxindoles are categorized based on their mentioned biological properties.

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Section: Synthetic Spirooxindolesmentioning

confidence: 99%

Spirooxindole: A Versatile Biologically Active Heterocyclic Scaffold

et al. 2023

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“…D. Rajaraman et al Reported a Synthesis, NMR, anti-oxidant, anti-cancer activity, Molecular docking, DFT Calculations, and in silico ADME analysis of 3'-benzoyl-4'-phenyl-5'-(piperazin-1ylmethyl)spiro[indoline-3,2'-pyrrolidin]-2-one derivatives. [21] In this research, they reported (figure 5) that a set of seven novel spirooxindole derivatives was synthesized through a three-component 1,3-dipolar cycloaddition method, involving the formation of azomethine ylides by combining isatin and amine with dipolarophile chalcones. These compounds demonstrated excellent antioxidant activity, particularly against hydroxyl and superoxide radicals, with IC50 values ranging from 15.9 to 30.3 μg/ml.…”

Section: Introductionmentioning

confidence: 99%

“…D. Rajaraman et al Reported a Synthesis, NMR, anti‐oxidant, anti‐cancer activity, Molecular docking, DFT Calculations, and in silico ADME analysis of 3′‐benzoyl‐4′‐phenyl‐5′‐(piperazin‐1‐ylmethyl)spiro[indoline‐3,2′‐pyrrolidin]‐2‐one derivatives [21] …”

Section: Introductionmentioning

confidence: 99%

Water‐Promoted Synthesis of Pyrazole‐Thiazole‐Derivatives as Potent Antioxidants And their Anti‐cancer Activity: ADMET and SAR Studies

Kachhot,

Vaghela,

Dhamal

et al. 2024

ChemistrySelect

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The hybridization of two drugs crizotinib and febuxostat was used for designing the molecules which were synthesized using the Hantzsch thiazole synthetic method. The reaction was improved using a variety of solvents. Nonetheless, the product was developed in aqueous conditions with a high yield (87 %). The explored approach has various benefits, including catalyst‐free synthesis, purification without column chromatography, and a greener solvent. The antioxidant potential was assessed by DPPH (1,1‐diphenyl‐2‐picrilhydrazyl) radical scavenging activity for compounds 7 a, 7 e, 7 g, 7 i, 7 j. The percentage of DPPH radical scavenging activity ranged from 20.674 to 59.083. The best antioxidant capacity was shown by 7 a (IC50=8.46); In addition, bioavailability was predicted for compound 7 a by in‐silico calculations of ADMET (absorption, distribution, metabolism, excretion, and toxicity) and pharmacokinetic parameters. A total of 10 thiazole derivatives were synthesized and out of which 05 compounds were evaluated for their anti‐cancer activity against 60 distinct human tumor cell lines. Most of the synthesised compounds show moderate to good anti‐cancer activity.

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