Current Strategies in Development of New Chromone Derivatives with Diversified Pharmacological Activities: A Review

Mohsin, Noor ul Amin; Irfan, Muhammad; Hassan, Shams Ul; Saleem, Usman

doi:10.1007/s11094-020-02187-x

Cited by 70 publications

(45 citation statements)

References 98 publications

(49 reference statements)

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“…Mechanistically, these compounds caused a cleavage in PARP-1 and activate caspase 7, resulting in morphological changes, such as bleb formation in the treated cells, and a significant increase in the nuclear fragmentation. Considering all the results, these findings demonstrate that these compounds (benzimidazole-piperazine hybrids) exert their cytotoxicity through the apoptotic cell death induction ( Özdemir et al, 2020 ).…”

Section: Mode Of Action As Anti-cancer Agentsmentioning

confidence: 72%

“…They evaluated protein–protein interactions in human embryonic kidney 293 (HEK-293) cells using protein-fragment complementation assays (PCA) to detect hidden or not expected biological functions from a wide variety of compounds, belonging to various therapeutic categories. PCA can identify unexpected anti-proliferative effects when using niclosamide, observed in various types of cancer cells, including a human prostate cancer cell (PC-3) ( Samy et al, 2020 ), a human lung cancer cell (A549) ( Özdemir, Turanli, Çalişkan, Arka, & Banoglu, 2020 ), a human pancreatic cancer cell (MiaPaCa) ( Lee, Lee, Sim, & Kim, 2020 ), a human colon cancer cell (LOVO) ( Lee et al, 2020 ), and a human glioblastoma cell (U87MG) ( Arzani et al, 2019 ), with an inhibitory concentration of 50 (IC 50 ) at the mean concentrations of 0.6 µM ( MacDonald et al, 2006 ). Since then, various preclinical studies (L. Chen et al, 2017 , Suliman et al, 2016 , Zhou et al, 2017 ) demonstrated that niclosamide exerts its anti-cancer effects through the inhibition of signaling pathways, including NOTCH, NF-κB, and mammalian target of rapamycin (mTOR).…”

Section: Mode Of Action As Anti-cancer Agentsmentioning

confidence: 99%

“…In parallel, AK301 induced the expression of tumor necrosis factor receptor 1 (TNFR1) therefore caused an increase in the susceptibility of cancer cells to apoptosis by TNF- α ( Laudisi et al, 2020 ). Özdemir et al ( Özdemir et al, 2020 ) developed a series of benzimidazole-piperazine hybrids and evaluated their toxicity effects against human lung cancer A549 and human breast cancer MCF-7 cells. The results demonstrated that most of the hybrids had anti-proliferative activity against A549 cells with the IC 50 of 2.8–7.8 µM.…”

Section: Mode Of Action As Anti-cancer Agentsmentioning

confidence: 99%

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Anthelmintics for drug repurposing: Opportunities and challenges

Alavi

Shahmabadi

2021

Saudi Pharmaceutical Journal

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Drug repositioning is defined as a process to identify a new application for drugs. This approach is critical as it takes advantage of well-known pharmacokinetics, pharmacodynamics, and toxicity profiles of the drugs; thus, the chance of their future failure decreases, and the cost of their development and the required time for their approval are reduced. Anthelmintics, which are antiparasitic drugs, have recently demonstrated promising anticancer effects in vitro and in vivo . This literature review focuses on the potential of anthelmintics for repositioning in the treatment of cancers. It also discusses their pharmacokinetics and pharmacodynamics as antiparasitic drugs, proposed anticancer mechanisms, present development conditions, challenges in cancer therapy, and strategies to overcome these challenges.

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Section: Mode Of Action As Anti-cancer Agentsmentioning

confidence: 72%

Section: Mode Of Action As Anti-cancer Agentsmentioning

confidence: 99%

Section: Mode Of Action As Anti-cancer Agentsmentioning

confidence: 99%

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Anthelmintics for drug repurposing: Opportunities and challenges

Alavi

Shahmabadi

2021

Saudi Pharmaceutical Journal

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“…Chromone is a natural compound present in the diet of humans and animals that has low toxicity to mammalian cells. 11 , 12 Previous studies have also shown that chromone derivatives possess a broad range of biological activities 13 depending on the substitution pattern of the chromone scaffold. 14 Maleimide is an important structural parent nucleus of a class of bioactive molecules and functional materials from Marine natural alkaloids.…”

Section: Introductionmentioning

confidence: 99%

Chromone Derivatives CM3a Potently Eradicate Staphylococcus aureus Biofilms by Inhibiting Cell Adherence

Zhan¹,

Xu²,

Zhan³

et al. 2021

IDR

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Introduction: The ability of Staphylococcus aureus to form biofilms is associated with high mortality and treatment costs. Established biofilms cannot be eradicated by many conventional antibiotics due to the development of antibiotic tolerance by S. aureus. Here we report the synthesis and biological characterization of novel small-molecule compounds with antibiofilm activity. Chromone 5-maleimide substitution compounds (CM3a) showed favorable antibacterial activity against S. aureus. Methods: CM3A with antibacterial activity was synthesized and screened. The minimum inhibitory concentration (MIC) of CM3a were determined by the broth microdilution method. Biofilm eradication assay and colony count methods were used to investigate the effect of CM3a on S. aureus biofilm disruption and killing. Changes in biofilm architecture when subjected to CM3a, were visualized using confocal laser scanning microscopy (CLSM). CCK-8 assay and survival rate of Galleria mellonella larvae were used to test the toxicity of CM3a. Results: The minimum inhibitory concentration (MIC) of CM3a against S. aureus was about 26.4 μM. Biofilm staining and laser scanning confocal microscopy analysis showed that CM3a eradicated S. aureus biofilms by reducing the viability of the constituent bacterial cells. On the other hand, CM3a showed negligible toxicity against mouse alveolar epithelial cells and Galleria mellonella larvae. Conclusion: Chromone derivatives CM3a has therapeutic potential as a safe and effective compound for the treatment of S. aureus infection.

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“…Chromones are a class of naturally occurring substances, widely distributed throughout nature, which has been recognized as a privileged structure for drug discovery since it has been associated with a variety of biological activities such as antifungal, antidiabetic, antiviral, and anti-hypertensive [7,8]. In addition, several molecules containing the chromone moiety display anti-inflammatory [9] and analgesic [10][11][12] activities.…”

Section: Introductionmentioning

confidence: 99%

5-O-methylcneorumchromone K Exerts Antinociceptive Effects in Mice via Interaction with GABAA Receptors

Opretzka

Freitas

Santo

et al. 2021

IJMS

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The proper pharmacological control of pain is a continuous challenge for patients and health care providers. Even the most widely used medications for pain treatment are still ineffective or unsafe for some patients, especially for those who suffer from chronic pain. Substances containing the chromone scaffold have shown a variety of biological activities, including analgesic effects. This work presents for the first time the centrally mediated antinociceptive activity of 5-O-methylcneorumchromone K (5-CK). Cold plate and tail flick tests in mice showed that the 5-CK-induced antinociception was dose-dependent, longer-lasting, and more efficacious than that induced by morphine. The 5-CK-induced antinociception was not reversed by the opioid antagonist naloxone. Topological descriptors (fingerprints) were employed to narrow the antagonist selection to further investigate 5-CK’s mechanism of action. Next, based on the results of fingerprints analysis, functional antagonist assays were conducted on nociceptive tests. The effect of 5-CK was completely reversed in both cold plate and tail-flick tests by GABAA receptor antagonist bicuculline, but not by atropine or glibenclamide. Molecular docking studies suggest that 5-CK binds to the orthosteric binding site, with a similar binding profile to that observed for bicuculline and GABA. These results evidence that 5-CK has a centrally mediated antinociceptive effect, probably involving the activation of GABAergic pathways.

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Current Strategies in Development of New Chromone Derivatives with Diversified Pharmacological Activities: A Review

Cited by 70 publications

References 98 publications

Anthelmintics for drug repurposing: Opportunities and challenges

Anthelmintics for drug repurposing: Opportunities and challenges

Chromone Derivatives CM3a Potently Eradicate Staphylococcus aureus Biofilms by Inhibiting Cell Adherence

5-O-methylcneorumchromone K Exerts Antinociceptive Effects in Mice via Interaction with GABAA Receptors

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