Exploration of (hetero)aryl Derived Thienylchalcones for Antiviral and Anticancer Activities

Patil, Vikrant; Patil, Siddappa A.; Patil, Renukadevi; Bugarin, Alejandro; Beaman, Kenneth D.; Patil, Shivaputra A.

doi:10.2174/1573406414666180524074648

Cited by 8 publications

(20 citation statements)

References 32 publications

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“…They reported two chalcone derivatives, isobavachalcone and helichrysetin, that exert prominent inhibitory activity against MERS-CoV 3CLpro (IC 50 : 35.85 and 67.04 lM, respectively) [20]. In the other study, chloropyridine chalcone derivative exhibited a better inhibitory activity against viral replication and cellular growth (EC 50 : 3.2 lg/mL; CC 50 : 5.5 lg/mL; SI 50 : 1.7 lg/mL), indicating that the pyridyl functionality can enhance anti-MERS-CoV activity [30]. Taken together, chalcone derivatives can target different types of CoVs, particularly their cysteine protease enzymes.…”

Section: Chalcone Derivatives Tested On Coronavirusesmentioning

confidence: 77%

“…These promising diverse antiviral bioactions, make chalcone derivatives a favourable broad-spectrum candidate for targeting the most recent viral pandemic, COVID-19 and any other potentially emerging viral diseases. Their interesting biological activities have been studied in several scientific investigations as potential pharmacological agents capable of targeting a variety of human viruses including; MERS-CoV, severe acute respiratory syndromerelated coronavirus (SARS-CoV), HIV, influenza virus, human rhinovirus, herpes simplex virus (HSV), dengue virus (DEN), human cytomegalovirus (HCMV), hepatitis B virus (HBV), hepatitis C virus (HCV), Rift Valley fever (RVF) and Venezuelan equine encephalitis virus (VEEV), through their well discovered antiviral cellular targets and based on specific chalcone skeleton design [20][21][22][23][24][25][26][27][28][29][30]. Figure 1 illustrates the main mechanisms of actions of chalcone derivatives that were reported in literature on different human viruses.…”

Section: Chalcones As Potential Candidates For Treating Viral Infectionsmentioning

confidence: 99%

“…They were also found to act on important receptors such as CXCR4 chemokine receptors [41], US28 receptor of HCMV [27] and capsid pocket inside viral protein 1 (VP1) in rhinovirus [42]. Other important activities include targeting the kinase activity of epidermal growth factor receptor (EGFR) [27], inhibition of DNA hybridisation [30], mammalian target of rapamycin (mTOR) pathway [43], blocking virus-mediated cell fusion and inhibiting the late stages of viral replication [44]. In addition, chalcones were demonstrated by some studies to act as broad-spectrum covering agents on different viral infections and were shown to possess some preventive and prophylactic potential [45].…”

Section: Chalcones As Potential Candidates For Treating Viral Infectionsmentioning

confidence: 99%

“…Chalcone pharmacophore represents a unique and attractive scaffold for the discovery and targeting of CoVs due to their significant anti-infective properties. Few chalcones were investigated with regards to their effect on CoVs infection, namely the SARS-CoV and MERS-CoV [20,21,30,47]. Only two studies investigated chalcones effect on SARS-CoV [21,47].…”

Section: Chalcone Derivatives Tested On Coronavirusesmentioning

confidence: 99%

“…Therefore, the substantial effect of chalones against these important proteases makes them attractive molecules for the development of anti-SARS drugs. On the other hand, two studies have explored chalcones activities against MERS-CoV [20,30]. MERS-CoV 3C-like protease (3CLpro) was explored as a target for chalones in a study published by Jo et al [20].…”

Section: Chalcone Derivatives Tested On Coronavirusesmentioning

confidence: 99%

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A comprehensive review on the antiviral activities of chalcones

Elkhalifa

Al-Hashimi

Moustafa

et al. 2020

Journal of Drug Targeting

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Some viral outbreaks have plagued the world since antiquity, including the most recent COVID-19 pandemic. The continuous spread and emergence of new viral diseases have urged the discovery of novel treatment options that can overcome the limitations of currently marketed antiviral drugs. Chalcones are natural open chain flavonoids that are found in various plants and can be synthesised in labs. Several studies have shown that these small organic molecules exert a number of pharmacological activities, including antiviral, anti-inflammatory, antimicrobial and anticancer. The purpose of this review is to provide a summary of the antiviral activities of chalcones and their derivatives on a set of human viral infections and their potential for targeting the most recent COVID-19 disease. Accordingly, we herein review chalcones activities on the following human viruses: Middle East respiratory syndrome coronavirus, severe acute respiratory syndrome coronavirus, human immunodeficiency, influenza, human rhinovirus, herpes simplex, dengue, human cytomegalovirus, hepatitis B and C, Rift Valley fever and Venezuelan equine encephalitis. We hope that this review will pave the way for the design and development of potentially potent and broad-spectrum chalcone based antiviral drugs.

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Section: Chalcone Derivatives Tested On Coronavirusesmentioning

confidence: 77%

Section: Chalcones As Potential Candidates For Treating Viral Infectionsmentioning

confidence: 99%

Section: Chalcones As Potential Candidates For Treating Viral Infectionsmentioning

confidence: 99%

Section: Chalcone Derivatives Tested On Coronavirusesmentioning

confidence: 99%

Section: Chalcone Derivatives Tested On Coronavirusesmentioning

confidence: 99%

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A comprehensive review on the antiviral activities of chalcones

Elkhalifa

Al-Hashimi

Moustafa

et al. 2020

Journal of Drug Targeting

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Madhuca indica: A Review on the Phytochemical and Pharmacological Aspects

et al. 2023

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Madhuca indica J.F. Gmel. (family: Sapotaceae), commonly known as Mahua in Indian dialects, occupies the importance as one of the fuel-efficient, energy-saving plant species. Extensive studies showed that the presence of phytochemicals e.g., carbohydrates, fatty acids, flavonoids, saponins, steroids, triterpenoids and glycosidic compounds in the extract of this species. Pharmacologically, it has been used against various disorders in indigenous system of medicine, inckuding antioxidant, anti-inflammatory, anticancer, hepatoprotective, anti-diabetic and wound healing activities. This review highlights various pharmacological activities, phytochemistry and importance of M. indica plant for medicine.

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In silico study of the potential interactions of 4′-acetamidechalcones with protein targets in SARS-CoV-2

Almeida-Neto

Matos

Marinho

et al. 2021

Biochemical and Biophysical Research Communications

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The sanitary emergency generated by the pandemic COVID-19, instigates the search for scientific strategies to mitigate the damage caused by the disease to different sectors of society. The disease caused by the coronavirus, SARS-CoV-2, reached 216 countries/territories, where about 20 million people were reported with the infection. Of these, more than 740,000 died. In view of the situation, strategies involving the development of new antiviral molecules are extremely important. The present work evaluated, through molecular docking assays, the interactions of 4′-acetamidechalcones with enzymatic and structural targets of SARS-CoV-2 and with the host's ACE2, which is recognized by the virus, facilitating its entry into cells. Therefore, it was observed that, regarding the interactions of chalcones with Main protease (Mpro), the chalcone N-(4′[(2E)-3-(4-flurophenyl)-1-(phenyl)prop-2-en-1-one]) acetamide (PAAPF) has the potential for coupling in the same region as the natural inhibitor FJC through strong hydrogen bonding. The formation of two strong hydrogen bonds between N-(4[(2E)-3-(phenyl)-1-(phenyl)-prop-2-en-1-one]) acetamide (PAAB) and the NSP16-NSP10 heterodimer methyltransferase was also noted. N-(4[(2E)-3-(4-methoxyphenyl)-1-(phenyl)prop-2-en-1-one]) acetamide (PAAPM) and N-(4-[(2E)-3-(4-ethoxyphenyl)-1-(phenyl)prop-2-en-1-one]) acetamide (PAAPE) chalcones showed at least one strong intensity interaction of the SPIKE protein. N-(4[(2E)-3-(4-dimetilaminophenyl)-1-(phenyl)-prop-2-en-1-one]) acetamide (PAAPA) chalcone had a better affinity with ACE2, with strong hydrogen interactions. Together, our results suggest that 4′-acetamidechalcones inhibit the interaction of the virus with host cells through binding to ACE2 or SPIKE protein, probably generating a steric impediment. In addition, chalcones have an affinity for important enzymes in post-translational processes, interfering with viral replication.

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Exploration of (hetero)aryl Derived Thienylchalcones for Antiviral and Anticancer Activities

Cited by 8 publications

References 32 publications

A comprehensive review on the antiviral activities of chalcones

A comprehensive review on the antiviral activities of chalcones

Madhuca indica: A Review on the Phytochemical and Pharmacological Aspects

In silico study of the potential interactions of 4′-acetamidechalcones with protein targets in SARS-CoV-2

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