Synthesis, Characterization and Anticancer Evaluation of Novel Analogues of Pyrazoles

Khatun, Babli; Kamath, Venkatesh; Muddukrishna, BS; Pai, Aravinda

doi:10.52711/0974-360x.2021.00382

Cited by 2 publications

(1 citation statement)

References 8 publications

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“…Studies have shown that some pyrazole derivatives have anticancer properties. For example, pyrazole is a pharmacophore for anticancer compounds such as Ruxolitinib (blood cancer), Axitinib (kidney cancer), and Crizotinib (lung cancer) [ 228 , 229 , 230 , 231 ].…”

Section: Synthetic Derivatives Of Chalcones With Anticancer Propertiesmentioning

confidence: 99%

Anticancer Activity of Natural and Synthetic Chalcones

Constantinescu

Lungu²

2021

IJMS

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Cancer is a condition caused by many mechanisms (genetic, immune, oxidation, and inflammatory). Anticancer therapy aims to destroy or stop the growth of cancer cells. Resistance to treatment is theleading cause of the inefficiency of current standard therapies. Targeted therapies are the most effective due to the low number of side effects and low resistance. Among the small molecule natural compounds, flavonoids are of particular interest for theidentification of new anticancer agents. Chalcones are precursors to all flavonoids and have many biological activities. The anticancer activity of chalcones is due to the ability of these compounds to act on many targets. Natural chalcones, such as licochalcones, xanthohumol (XN), panduretin (PA), and loncocarpine, have been extensively studied and modulated. Modification of the basic structure of chalcones in order to obtain compounds with superior cytotoxic properties has been performed by modulating the aromatic residues, replacing aromatic residues with heterocycles, and obtaining hybrid molecules. A huge number of chalcone derivatives with residues such as diaryl ether, sulfonamide, and amine have been obtained, their presence being favorable for anticancer activity. Modification of the amino group in the structure of aminochalconesis always favorable for antitumor activity. This is why hybrid molecules of chalcones with different nitrogen hetercycles in the molecule have been obtained. From these, azoles (imidazole, oxazoles, tetrazoles, thiazoles, 1,2,3-triazoles, and 1,2,4-triazoles) are of particular importance for the identification of new anticancer agents.

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Section: Synthetic Derivatives Of Chalcones With Anticancer Propertiesmentioning

confidence: 99%

Anticancer Activity of Natural and Synthetic Chalcones

Constantinescu

Lungu²

2021

IJMS

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COVID-19 Activity of Some 9-Anilinoacridines substituted with Pyrazole against SARS CoV2 Main Protease: An In-silico Approach

Rajagopal

Kannan

Aparna

et al. 2023

RJPT

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COVID-19 is affected in more than 200 countries in the world. In this article, some pyrazole bearing 9-anilinoacridines(1a-z) were designed by in-silico studies for SARS-CoV-2 Mpro inhibitory activity. The docking for 1a-z against SARS-CoV-2 Mpro (5R82.pdb) targeting corona virus using Schrodinger suit. The Glide module is used for docking, qikprop for in-silico ADMET screening and Prime MM-GB/SA to determine binding energy of ligands. From the results, many compounds are significantly binding with SARS-CoV-2 Mpro with high G-score when compared to one of the currently recommended drug for COVID19, Hydroxychloroquine (-5.47). From results, many compounds exhibited similar interactions with SARS-CoV-2 Mpro and the aminoacids between GLN19 and GLY143 plays major role for binding. The in-silico ADMET properties are within the recommended values. The MM-GBSA calculations for most of the potent inhibitors are stable. In conclusion, 1t,m,j,o are SARS-CoV-2 Mpro inhibitors and may be useful for significant COVID19 activity after further refinement.

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Synthesis, Characterization and Anticancer Evaluation of Novel Analogues of Pyrazoles

Cited by 2 publications

References 8 publications

Anticancer Activity of Natural and Synthetic Chalcones

Anticancer Activity of Natural and Synthetic Chalcones

COVID-19 Activity of Some 9-Anilinoacridines substituted with Pyrazole against SARS CoV2 Main Protease: An In-silico Approach

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