Novel imidazole derivatives as potential aromatase and monoamine oxidase-B inhibitors against breast cancer

Osmaniye, Derya; Levent, Serkan; Sağlık, Begüm Nurpelin; Karaduman, Abdullah Burak; Özkay, Yusuf; Kaplancıklı, Zafer Asım

doi:10.1039/d2nj00424k

Cited by 11 publications

(8 citation statements)

References 43 publications

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“…Inhibition % at all concentrations was determined using the formula below, and the IC 50 values were calculated from a dose–response curve obtained by plotting the percentage inhibition versus the log concentration with the use of Microsoft Excel 2013. The results were displayed as mean ± standard deviation (SD). − …”

Section: Methodsmentioning

confidence: 99%

“…Since targeting human aromatase enzyme was reported for antifungal activity and it plays a pivotal role in fungal cell function, compounds that showed antifungal activity were evaluated for inhibition activity on aromatase enzyme using a kit procedure (Bio Vision, Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric)), as described in previous studies. − …”

Section: Methodsmentioning

confidence: 99%

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Investigation of Novel Quinoline–Thiazole Derivatives as Antimicrobial Agents: In Vitro and In Silico Approaches

et al. 2022

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Infectious diseases are a major concern around the world. Today, it is an urgent need for new chemotherapeutics for infectious diseases. Because of that, our group designed, synthesized, and analyzed 14 new quinoline derivatives endowed with the pharmacophore moiety of fluoroquinolones primarily for their antimicrobial effects. Their cytotoxicity effects were tested against six bacterial and four fungal strains and NIH/3T3 cell line. Additionally, their action mechanisms were evaluated against DNA gyrase and lanosterol 14α-demethylase (LMD). Furthermore, to eliminate the potential side effects, the active compounds were evaluated against the aromatase enzyme. The experimental enzymatic results were evaluated for active compounds’ binding modes using molecular docking and molecular dynamics simulation studies. The results were utilized to clarify the structure–activity relationship (SAR). Finally, compound 4m was the most potent compound for its antifungal activity with low cytotoxicity against healthy cells and fewer possible side effects, while compounds 4j and 4l can be used alone for special patients who are suffering from fungal infections in addition to the primer disease.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Investigation of Novel Quinoline–Thiazole Derivatives as Antimicrobial Agents: In Vitro and In Silico Approaches

et al. 2022

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“…The aromatase inhibitory activity of compound 82 had an IC 50 value of 20 nM. The reference drug used in the study was letrozole (IC 50 = 24 nM) [ 64 ].…”

Section: Aromatase Inhibitorsmentioning

confidence: 99%

Aromatase Inhibitors as a Promising Direction for the Search for New Anticancer Drugs

Janowska,

Holota,

Lesyk

et al. 2024

Molecules

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Aromatase is an enzyme that plays a crucial role in the biosynthesis of estrogens, which are hormones that contribute to the growth of certain types of breast cancer. In particular, aromatase catalyzes the conversion of androgens (male hormones) into estrogens (female hormones) in various tissues, including the adrenal glands, ovaries, and adipose tissue. Given the role of estrogen in promoting the growth of hormone-receptor-positive breast cancers, aromatase has become an important molecular target for the development of anticancer agents. Aromatase inhibitors can be classified into two main groups based on their chemical structure: steroidal and non-steroidal inhibitors. This work presents a review of the literature from the last ten years regarding the search for new aromatase inhibitors. We present the directions of search, taking into account the impact of structure modifications on anticancer activity.

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“…Furthermore, these compounds have been investigated for their potential in targeting insulin-linked cancer cells (insulin receptor-A and IGF-1R and their heterodimers [ 35 , 36 ]). They have also been explored for hormonal-based targeting of cancer cells (estrogen-based drugs targeting breast cancer [ 37 , 38 , 39 , 40 , 41 ]).…”

Section: Introductionmentioning

confidence: 99%

Imidazoles as Serotonin Receptor Modulators for Treatment of Depression: Structural Insights and Structure–Activity Relationship Studies

Goel,

Thapliyal,

Kharb

et al. 2023

Pharmaceutics

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Serotoninergic signaling is identified as a crucial player in psychiatric disorders (notably depression), presenting it as a significant therapeutic target for treating such conditions. Inhibitors of serotoninergic signaling (especially selective serotonin reuptake inhibitors (SSRI) or serotonin and norepinephrine reuptake inhibitors (SNRI)) are prominently selected as first-line therapy for the treatment of depression, which benefits via increasing low serotonin levels and norepinephrine by blocking serotonin/norepinephrine reuptake and thereby increasing activity. While developing newer heterocyclic scaffolds to target/modulate the serotonergic systems, imidazole-bearing pharmacophores have emerged. The imidazole-derived pharmacophore already demonstrated unique structural characteristics and an electron-rich environment, ultimately resulting in a diverse range of bioactivities. Therefore, the current manuscript discloses such a specific modification and structural activity relationship (SAR) of attempted derivatization in terms of the serotonergic efficacy of the resultant inhibitor. We also featured a landscape of imidazole-based development, focusing on SAR studies against the serotoninergic system to target depression. This study covers the recent advancements in synthetic methodologies for imidazole derivatives and the development of new molecules having antidepressant activity via modulating serotonergic systems, along with their SAR studies. The focus of the study is to provide structural insights into imidazole-based derivatives as serotonergic system modulators for the treatment of depression.

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Novel imidazole derivatives as potential aromatase and monoamine oxidase-B inhibitors against breast cancer

Abstract: In this study, we developed a series of new aromatase MAO -B dual inhibitors against breast cancer. Aromatase inhibitors are the most commonly used drugs clinically for breast cancer. In...

Cited by 11 publications

References 43 publications

Investigation of Novel Quinoline–Thiazole Derivatives as Antimicrobial Agents: In Vitro and In Silico Approaches

Investigation of Novel Quinoline–Thiazole Derivatives as Antimicrobial Agents: In Vitro and In Silico Approaches

Aromatase Inhibitors as a Promising Direction for the Search for New Anticancer Drugs

Imidazoles as Serotonin Receptor Modulators for Treatment of Depression: Structural Insights and Structure–Activity Relationship Studies

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