Synthetic approach toward spiro quinoxaline-β-lactam based heterocyclic compounds: Spectral characterization, SAR, pharmacokinetic and biomolecular interaction studies

Dabhi, Ravi A.; Dhaduk, Milan P.; Bhatt, Vaibhav D.; Bhatt, Bhupesh S.

doi:10.1080/07391102.2022.2086176

Cited by 12 publications

(1 citation statement)

References 55 publications

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“…Absorption, distribution, metabolism, and excretion (ADME) analysis predict the druggability of a molecule by studying its adherence with the ‘Lipinski Five’ Rules [ 60 ]. The pharmacokinetic properties and drug-likeness of novel amidic derivatives of Quinazolinone ( 7a-j ) were studied and compared with standard drug (Etoposide) using an online accessible web tool: ADMET lab 2.0 and SwissADME program of the Molecular Modelling Group of the Swiss Institute of Bioinformatics [ [61] , [62] , [63] , [64] , [65] , [66] ] which are publicly available at https://admet mesh.scbdd.com and http://www . Swissadme.ch, respectively.…”

Section: Resultsmentioning

confidence: 99%

Design, synthesis, in-silico studies and apoptotic activity of novel amide enriched 2-(1H)- quinazolinone derivatives

Gariganti,

Bandi,

Gatta

et al. 2024

Heliyon

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Section: Resultsmentioning

confidence: 99%

Design, synthesis, in-silico studies and apoptotic activity of novel amide enriched 2-(1H)- quinazolinone derivatives

Gariganti,

Bandi,

Gatta

et al. 2024

Heliyon

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Calix[4]pyrrole‐Grafted Gold Nanoparticles as a Turn‐On Fluorescence Sensor for Noxious Fungicide Dimoxystrobin and Their Anti‐Cancer Activity against the KB‐3‐1 Cell Line

Pomal

Bhatt

Kundariya³

et al. 2023

ChemistrySelect

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A rapid and easy approach for producing very stable gold nanoparticles has been discovered. Calix[4]pyrrole tetrahydrazide (CPTAH) was utilized effectively in the synthesis of gold nanoparticles as a reducing and stabilizing agent. These functionalized AuNPs were characterized by Surface Plasmon Resonance, Transmission Electron Microscopy, Selected Area Electron Diffraction, and Energy Dispersive X‐ray techniques. CPTAH‐AuNPs possessed a particle size of 11±2 nm and are highly stable at pH 7.0 for more than 150 days. The selectivity and sensitivity of CPTAH‐AuNPs as a fungicide sensor was assessed for Metalaxyl, Mancozeb, Tebuconazole, Tricyclozole, Dimoxystrobin, Kresoxim‐methyl, and Carbendazim, amongst which Dimoxystrobin (DMX) was sensed exclusively with naked eyes by means of aggregation of CPTAH‐AuNPs with a detection limit of the order of 5 ppm using “Turn‐on” fluorescence enhancement. Additionally, the CPTAH‐AuNPs were found to be effective cytotoxic agent against the human cervix cancer cell line KB‐3‐1 with IC50 value of 64.63 μg/mL which admits the employability of CPTAH‐AuNPs in the study of development of anti‐cancer drug.

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Anticancer Potential of Quinazoline Derivatives Modified with Hydrazones and Triazoles Against MG‐63 Cancer Cell Line

Kumar,

Kamal

et al. 2024

ChemistrySelect

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Antiproliferative potential of quinazoline flanked bis‐hydrazones and quinazoline fused bis‐triazoles against human bone cancer cell line (MG‐63) have been described in the present work. A series of 2,4‐bis(2‐(E)‐arylidenehydrazinyl)quinazolines 5a–5n have been synthesized by refluxing 2,4‐dihydrazinylquinazoline with respective benzaldehyde derivatives. Thereafter, these bis‐hydrazone derivatives 5a–5n have been cyclized to corresponding 3,7‐diarylbis([1,2,4]triazolo)[4,3‐a][4′,3′‐c]quinazolines 6a–6n by using bis(trifluoroacetoxy)iodobenzene (PIFA) as oxidant. All the synthesized bis‐hydrazones 5a–5n and bis‐triazoles 6a–6n were tested for their in vitro anticancer potential against human bone cancer cell line, i.e., MG‐63. These compounds demonstrated moderate to significant cytotoxic activities against the tested cancer cell line comparable to camptothecin as a standard. However, the bis‐hydrazones, 5i and 5n displayed potent antiproliferative properties with GI50 values of 114.31 µM and 136.95 µM, respectively and bis‐triazoles, 6i and 6k may be considered as potent antiproliferative agents with their GI50 values 137.69 µM and 124.26 µM, respectively.

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Synthetic approach toward spiro quinoxaline-β-lactam based heterocyclic compounds: Spectral characterization, SAR, pharmacokinetic and biomolecular interaction studies

Cited by 12 publications

References 55 publications

Design, synthesis, in-silico studies and apoptotic activity of novel amide enriched 2-(1H)- quinazolinone derivatives

Design, synthesis, in-silico studies and apoptotic activity of novel amide enriched 2-(1H)- quinazolinone derivatives

Calix[4]pyrrole‐Grafted Gold Nanoparticles as a Turn‐On Fluorescence Sensor for Noxious Fungicide Dimoxystrobin and Their Anti‐Cancer Activity against the KB‐3‐1 Cell Line

Anticancer Potential of Quinazoline Derivatives Modified with Hydrazones and Triazoles Against MG‐63 Cancer Cell Line

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