Design, Synthesis, Characterization, Evaluation for Anticancer and Cytotoxic Properties of New Pyrazole Carbothioamides

Kumar, A. Dileep; Vagish, C.B.; Lokeshwari, Devirammanahalii Mahadevaswamy; Sowmya, R; Kumar, K. Ajay

doi:10.14233/ajomc.2021.ajomc-p291

Cited by 3 publications

(1 citation statement)

References 27 publications

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“…The pyrazole derivatives were prepared in good to excellent chemical yields by the silver chloride catalyzed isomerization of α , β -acetylenic hydrazones in dichloromethane at room temperature [ 3 ]. The molecular iodine catalyzed reaction of α,β-unsaturated ketones and sulfonyl hydrazide [ 4 ], the four-component reaction of dialkyl acetylenedicarboxylates, isocyanides, ethyl acetoacetate and hydrazine/phenylhydrazine produce pyrazoles [ 5 ], The (3 + 2) annulation of chalcones with thiosemicarbazide [ 6 ], and hydrazines with ynone trifluoroborates [ 7 ] gave pyrazoles with regioselectivity. The Chloramine-T catalyzed 1,3-dipolar cycloaddition of hydrazones to alkenes form pyrazoles [ 8 ].…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, characterization, and antioxidant activity studies of novel thienyl-pyrazoles

Kumara

Prabhudeva

Vagish

et al. 2021

Heliyon

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In a sustained search for novel and effective antioxidants, a potential therapeutic leads against renal, and neurological disorders. Amongst the heterocycles, pyrazole and their derivatives have been extensively studied for their biological potencies, particularly to a larger extent for their antioxidant properties. Although many of pyrazole derivatives displayed antioxidant activities, still there is a need of developing efficient protocol for their synthesis, involving ecofriendly conditions, molecules of greater antioxidant efficacy and lesser toxicity, etc. In this context, the current study presents an amberlyst-15 catalysed efficient synthesis of 2-pyrazoline derivatives, 5 ( a - g ) via (3 + 2) annulation of chalcones with phenylhydrazines. Structure proofs of new pyrazoles offered by spectral studies, and the molecular structure of compound 5d of the series by crystallographic studies, which revealed an intra molecular hydrogen bond interactions (C–H⋯N type), and stabilization by C–H...π and π---π molecular interactions. Of the series, compounds 5g and 5h show excellent DPPH (IC 50 = 0.245 ± 0.01, and 0.284 ± 0.02 μM); and hydroxyl (IC 50 = 0.905 ± 0.01, and 0.892 ± 0.01μM) radical scavenging activities comparable with respective controls, ascorbic acid (IC 50 = 0.483 ± 0.01μM) and BHA (IC 50 = 1.739 ± 0.01μM). The molecular docking and ADME/Tox studies indicate that, these compounds have good antioxidant activity through π-π stacking with Catalase via Try337 and Phe140, and therefore, might be lead antioxidants for further study.

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Section: Introductionmentioning

confidence: 99%

Design, synthesis, characterization, and antioxidant activity studies of novel thienyl-pyrazoles

Kumara

Prabhudeva

Vagish

et al. 2021

Heliyon

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Synthetic Strategies of Pyrazoline Derivatives for the Development of New Anticancer Agents: Recent Updates

Ray¹,

Salahuddin²,

Mazumder³

et al. 2024

MROC

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Background: Pyrazoline is a heterocyclic compound of five rings, three carbon atoms, and two nitrogen atoms in a circle with just one endocyclic bond. Pyrazoline is one form of electron-rich nitrogen carrier, gaining popularity because it combines exciting electronic properties with the potential for dynamic applications. Many methods have been used in this research to synthesize pyrazoline derivatives to show a highly biological effect. Objective: The research of pyrazoline derivatives' biological activity has been a fascinating area of pharmaceutical chemistry. Pyrazolines are used in multifunctional applications. The current review of pyrazoline derivatives patent literature (2000-2021) describing the introduction, general method, and synthetic scheme on Anticancer activity has been discussed. Conclusion: Pyrazolines is a known heterocyclic compound. Pyrazoline is a five-membered ring containing three carbon and two nitrogen atoms nearby. Many approaches can be used to figure out their Synthesis. Numerous pyrazoline derivatives have been discovered to have an essential biological effect on anticancer activity, which has encouraged research in this area. The use of pyrazoline against cancer is a brilliant moiety and has an enormous scope of interest for the researchers to search more about this moiety.

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An Insight into Pyrazole-containing Compounds: Synthesis and Pharmacological Activities

Kumar

Bansal

Goyal

2022

AIA

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Background: Heterocyclic scaffolds have gained exceptional devotion in the recent years due to their marked utility in bio-organic field. Among these, pyrazole remains a privileged scaffold as broad array of medicinally active agents encompasses this heterocycle as a core nucleus. Pyrazole is a five-membered, aromatic ring containing two nitrogen atoms at adjacent positions are readily able to show interactions with numerous receptor (s), enzymes located on the target cells in biological system. Pyrazole-containing compounds are acknowledged with anticyclooxygenases (anti-inflammatory), carbonic anhydrase inhibitor, α-glycosidase inhibitor, and cholinesterase enzymes inhibitor and anti-DNA gyrases activities. Noticeably, rimonabant, phenylbutazone, fipronil, difenamizole, celecoxib, antipyrine, fezolamide and betazole are few representatives of pyrazole containing drugs. Objectives: The manuscript aims to review the detailed synthetic approaches applied for the synthesis of pyrazole derivatives. In particular, we examine recent scientific finding on antimicrobial, anti-tubercular, antiviral, anticancer and anti-inflammatory perspectives of pyrazole containing analogues. Methods: Pyrazole analogues have been widely explored by scientific community as large number of papers has been published in this regard. Numerous pyrazole-containing analogues have been designed, synthesized, and screened for their in vitro and in vivo bio-efficacy and many of them endowed with commendable pharmacological activities. Pyrazole analogues with superior applications as antiviral, anticancer, and anti-inflammatory efficacy have also been well documented in patents granted to this heterocyclic nucleus. Results: This review outlines the recent advances in medicinal chemistry of pyrazole analogues with a special emphasize of structure-activity relationships to afford ideas for the rational drug-design and discovery and their impact on desired pharmacological applications. Conclusion: The information provided in this manuscript may help the medicinal chemists to generate robust pyrazole analogues with high efficacy.

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Design, Synthesis, Characterization, Evaluation for Anticancer and Cytotoxic Properties of New Pyrazole Carbothioamides

Cited by 3 publications

References 27 publications

Design, synthesis, characterization, and antioxidant activity studies of novel thienyl-pyrazoles

Design, synthesis, characterization, and antioxidant activity studies of novel thienyl-pyrazoles

Synthetic Strategies of Pyrazoline Derivatives for the Development of New Anticancer Agents: Recent Updates

An Insight into Pyrazole-containing Compounds: Synthesis and Pharmacological Activities

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