Ekta Lathwal - Academia.edu (original) (raw)

Papers by Ekta Lathwal

Research paper thumbnail of A Review of the Various Synthetic Approaches to Access Aurone Derivatives and their Biological Activities

Current Organic Chemistry

: Aurones, a member of the flavonoid family, have limited occurrence in nature and are relatively... more : Aurones, a member of the flavonoid family, have limited occurrence in nature and are relatively less explored than other flavonoids but still constitute a gleaming class of therapeutically significant oxygen heterocyclic molecules with broad-spectrum biological activities. These are secondary plant metabolites and are responsible for glaring pigmentation to various colored parts of the plants. This review covers the comprehensive history of aurones from 1918 to 2020. This review provides a generalized and systematic study of the protocols adopted for synthesizing aurone derivatives and their biological profile. Though there are many review articles on the biological activities of aurones, none of these cover the synthetic aspects of the protocols thoroughly. With the growing number of biologically active natural and synthesized aurones, a massive breakthrough in aurone research has emerged, and it is now one of the most researched O-heterocycles. The present review aims to highlight the work of the researchers on aurones to help synthetic chemists and future generations to design and develop new aurone-based heterocyclic systems of therapeutic potential. This review will also catch the attention of researchers for exploring various other potentials of aurones.

Research paper thumbnail of Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, 2016

A series of 4-phthalimidobenzenesulfonamide derivatives were designed, synthesized and evaluated ... more A series of 4-phthalimidobenzenesulfonamide derivatives were designed, synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Structures of the title compounds were confirmed by spectral and elemental analyses. The cholinesterase (ChE) inhibitory activity studies were carried out using Ellman's colorimetric method. The biological activity results revealed that all of the title compounds (except for compound 8) displayed high selectivity against AChE. Among the tested compounds, compound 7 was found to be the most potent against AChE (IC 50 ¼ 1.35 ± 0.08 lM), while compound 3 exhibited the highest inhibition against BuChE (IC 50 ¼ 13.41 ± 0.62 lM). Molecular docking studies of the most active compound 7 in AChE showed that this compound can interact with both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE.

Research paper thumbnail of An ultrasound-assisted three component protocol for the regio and stereo-selective synthesis of some novel dispiroheterocycles and their biological evaluation as anti-inflammatory, anti-obesity agents

Letters in Drug Design & Discovery, Mar 6, 2023

Research paper thumbnail of Recent Developments in Nanocatalyzed Green Synthetic Protocols of Biologically Potent Diverse O-Heterocycles—A Review

Catalysts

The dynamic growth in green organic synthetic methodologies for diverse heterocyclic scaffolds ha... more The dynamic growth in green organic synthetic methodologies for diverse heterocyclic scaffolds has substantially contributed to the field of medicinal chemistry over the last few decades. The use of hybrid metal nanocatalysts (NCs) is one such benign strategy for ensuring the advancement of modern synthetic chemistry by adhering to the principles of green chemistry, which call for a sustainable catalytic system that converts reacting species into profitable chemicals at a faster rate and tends to reduce waste generation. The metal nanoparticles (NPs) enhance the exposed surface area of the catalytic active sites, thereby making it easier for reactants and metal NCs to have an effective interaction. Several review articles have been published on the preparation of metal NCs and their uses for various catalytic heterocyclic transformations. This review will summarize different metal NCs for the efficient green synthesis of various O-heterocycles. Furthermore, the review will provide a...

Research paper thumbnail of Synthesis, cytotoxic evaluation and structure activity relationship of pyrazole hybrid aurones on gastric cancer (AGS) cell lines

Research paper thumbnail of Synthesis of propynyloxy substituted some novel aurones as potent Cathepsin B inhibitors

Chemical Data Collections, 2020

Abstract A two-step synthesis was designed to develop a novel series of 6-propynyloxyaurones, 2(a... more Abstract A two-step synthesis was designed to develop a novel series of 6-propynyloxyaurones, 2(a-r). The synthesized aurone derivatives were characterized by their IR, NMR, and mass spectrometry data. The present study proposes these aurones as anti-inflammatory and anti-Alzheimer candidates on the basis of their cathepsin B inhibitory activities. Anti-cathepsin activity of some of the synthesized aurones was found, either equivalent to or higher than the reference drugs, aspirin and curcumin at submicromolar concentrations. Among the studied compounds, 2e, 2i, 2n, 2q, and 2r exhibited much higher activity in comparison to the standard drugs. The molecular docking study also highlighted compound 2r for its greater anti-cathepsin B activity among all the designed aurones.

Research paper thumbnail of Synthesis of pyrazole based novel aurone analogs and their cytotoxic activity against MCF-7 cell line

Chemical Data Collections

Abstract A series of pyrazole based aurone analogs 3(a-n) have been synthesized and evaluated for... more Abstract A series of pyrazole based aurone analogs 3(a-n) have been synthesized and evaluated for their cytotoxic activity against MCF-7 cell line. All the products have been obtained by solid phase reaction and organic solvent free simple work-up procedure. Structures of the synthesized aurones were confirmed by their IR, 1H-NMR, 13C-NMR, elemental analysis and mass spectrometry data. The cytotoxic activity of these compounds was assessed by MTT assay and the nine products were found to be potential inhibitors against human breast adenocarcinoma cell line i.e. MCF-7. Aurone analogs 3a, 3b, 3c, 3e, 3i and 3n are the most active against the MCF-7 cell line with IC50 of 13.8, 15.8, 4.3, 2.7, 12.9 and 15.5μg/mL respectively, as compared to paclitaxel, with an IC50 value of 18.5μg/mL. Cytotoxicity against MCF-7 cancer cells, makes these molecules attractive candidates for the potential anticancer drug.

Research paper thumbnail of Synthesis and Biological Evaluation of Quinoline‐Based Novel Aurones

Research paper thumbnail of A Review of the Various Synthetic Approaches to Access Aurone Derivatives and their Biological Activities

Current Organic Chemistry

: Aurones, a member of the flavonoid family, have limited occurrence in nature and are relatively... more : Aurones, a member of the flavonoid family, have limited occurrence in nature and are relatively less explored than other flavonoids but still constitute a gleaming class of therapeutically significant oxygen heterocyclic molecules with broad-spectrum biological activities. These are secondary plant metabolites and are responsible for glaring pigmentation to various colored parts of the plants. This review covers the comprehensive history of aurones from 1918 to 2020. This review provides a generalized and systematic study of the protocols adopted for synthesizing aurone derivatives and their biological profile. Though there are many review articles on the biological activities of aurones, none of these cover the synthetic aspects of the protocols thoroughly. With the growing number of biologically active natural and synthesized aurones, a massive breakthrough in aurone research has emerged, and it is now one of the most researched O-heterocycles. The present review aims to highlight the work of the researchers on aurones to help synthetic chemists and future generations to design and develop new aurone-based heterocyclic systems of therapeutic potential. This review will also catch the attention of researchers for exploring various other potentials of aurones.

Research paper thumbnail of Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, 2016

A series of 4-phthalimidobenzenesulfonamide derivatives were designed, synthesized and evaluated ... more A series of 4-phthalimidobenzenesulfonamide derivatives were designed, synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Structures of the title compounds were confirmed by spectral and elemental analyses. The cholinesterase (ChE) inhibitory activity studies were carried out using Ellman's colorimetric method. The biological activity results revealed that all of the title compounds (except for compound 8) displayed high selectivity against AChE. Among the tested compounds, compound 7 was found to be the most potent against AChE (IC 50 ¼ 1.35 ± 0.08 lM), while compound 3 exhibited the highest inhibition against BuChE (IC 50 ¼ 13.41 ± 0.62 lM). Molecular docking studies of the most active compound 7 in AChE showed that this compound can interact with both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE.

Research paper thumbnail of An ultrasound-assisted three component protocol for the regio and stereo-selective synthesis of some novel dispiroheterocycles and their biological evaluation as anti-inflammatory, anti-obesity agents

Letters in Drug Design & Discovery, Mar 6, 2023

Research paper thumbnail of Recent Developments in Nanocatalyzed Green Synthetic Protocols of Biologically Potent Diverse O-Heterocycles—A Review

Catalysts

The dynamic growth in green organic synthetic methodologies for diverse heterocyclic scaffolds ha... more The dynamic growth in green organic synthetic methodologies for diverse heterocyclic scaffolds has substantially contributed to the field of medicinal chemistry over the last few decades. The use of hybrid metal nanocatalysts (NCs) is one such benign strategy for ensuring the advancement of modern synthetic chemistry by adhering to the principles of green chemistry, which call for a sustainable catalytic system that converts reacting species into profitable chemicals at a faster rate and tends to reduce waste generation. The metal nanoparticles (NPs) enhance the exposed surface area of the catalytic active sites, thereby making it easier for reactants and metal NCs to have an effective interaction. Several review articles have been published on the preparation of metal NCs and their uses for various catalytic heterocyclic transformations. This review will summarize different metal NCs for the efficient green synthesis of various O-heterocycles. Furthermore, the review will provide a...

Research paper thumbnail of Synthesis, cytotoxic evaluation and structure activity relationship of pyrazole hybrid aurones on gastric cancer (AGS) cell lines

Research paper thumbnail of Synthesis of propynyloxy substituted some novel aurones as potent Cathepsin B inhibitors

Chemical Data Collections, 2020

Abstract A two-step synthesis was designed to develop a novel series of 6-propynyloxyaurones, 2(a... more Abstract A two-step synthesis was designed to develop a novel series of 6-propynyloxyaurones, 2(a-r). The synthesized aurone derivatives were characterized by their IR, NMR, and mass spectrometry data. The present study proposes these aurones as anti-inflammatory and anti-Alzheimer candidates on the basis of their cathepsin B inhibitory activities. Anti-cathepsin activity of some of the synthesized aurones was found, either equivalent to or higher than the reference drugs, aspirin and curcumin at submicromolar concentrations. Among the studied compounds, 2e, 2i, 2n, 2q, and 2r exhibited much higher activity in comparison to the standard drugs. The molecular docking study also highlighted compound 2r for its greater anti-cathepsin B activity among all the designed aurones.

Research paper thumbnail of Synthesis of pyrazole based novel aurone analogs and their cytotoxic activity against MCF-7 cell line

Chemical Data Collections

Abstract A series of pyrazole based aurone analogs 3(a-n) have been synthesized and evaluated for... more Abstract A series of pyrazole based aurone analogs 3(a-n) have been synthesized and evaluated for their cytotoxic activity against MCF-7 cell line. All the products have been obtained by solid phase reaction and organic solvent free simple work-up procedure. Structures of the synthesized aurones were confirmed by their IR, 1H-NMR, 13C-NMR, elemental analysis and mass spectrometry data. The cytotoxic activity of these compounds was assessed by MTT assay and the nine products were found to be potential inhibitors against human breast adenocarcinoma cell line i.e. MCF-7. Aurone analogs 3a, 3b, 3c, 3e, 3i and 3n are the most active against the MCF-7 cell line with IC50 of 13.8, 15.8, 4.3, 2.7, 12.9 and 15.5μg/mL respectively, as compared to paclitaxel, with an IC50 value of 18.5μg/mL. Cytotoxicity against MCF-7 cancer cells, makes these molecules attractive candidates for the potential anticancer drug.

Research paper thumbnail of Synthesis and Biological Evaluation of Quinoline‐Based Novel Aurones