Sirtuin inhibition and anti-cancer activities of ethyl 2-benzimidazole-5-carboxylate derivatives

Yoon, Yeong Keng; Azizi, Mohamed Iman Hidayat Nor; Berdigaliyev, Nurken; Chen, Win Ning; Lee, W. L.; Shirazi, Amir Nasrolahi; Parang, Keykavous

doi:10.1039/c9md00323a

Cited by 15 publications

(13 citation statements)

References 27 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Among the cell lines evaluated, H103 showed a high sensitivity for BZD9Q1 and induced a prominent G2/M cell cycle arrest and apoptosis in these cells (Yeong et al, 2019). SIRT3 overexpression has been reported in HSC-3, UM-SCC-1, and UM-SCC-17B OSCC cell lines.…”

Section: Sirt3 In Oral Cancermentioning

confidence: 91%

“…Till date, not even a single study reported the role of SIRT2 in oral cancer. Upregulation of SIRT3 has been observed in several OSCC cell lines and in OSCC tissue samples (Alhazzazi et al., 2011; Yeong et al., 2019). Till date, in the context of oral cancer, only a few studies have reported the role of SIRT1 and 3, and therefore, the results of such studies are not conclusive.…”

Section: Sirtuins: Types Location and Functionsmentioning

confidence: 99%

“…In a study, BZD9Q1, a synthesized SIRT3 inhibitor, has been studied against human OSCC cell lines such as CCRF‐CEM, HCT‐116, H103, and MDA‐MB‐468. Among the cell lines evaluated, H103 showed a high sensitivity for BZD9Q1 and induced a prominent G2/M cell cycle arrest and apoptosis in these cells (Yeong et al., 2019). SIRT3 overexpression has been reported in HSC‐3, UM‐SCC‐1, and UM‐SCC‐17B OSCC cell lines.…”

Section: Sirt1 In Oral Cancermentioning

confidence: 99%

See 2 more Smart Citations

The ambiguous role of sirtuins in head and neck squamous cell carcinoma

et al. 2021

View full text Add to dashboard Cite

Oral cancer is one of the most leading cancer responsible for significant morbidity and mortality. The sirtuins (SIRTs) are a family of class III histone deacetylases and are known to regulate a variety of molecular signaling associated with different cancer types including oral malignancies. SIRT1 acts as bifunctional in a variety of cancer. In oral cancer, SIRT1 seems to work as a tumor suppressor. The carcinogenic potential of SIRT1 is also reported in oral cancer, and hence, its role is still ambiguous.SIRT2 is also said to play a dual-faced role in different types of cancers. However, in oral cancer, SIRT2 is not studied and its role remains obscure. SIRT3 expression was positively correlated with oral malignancies. However, studies also showed the anticancer role of SIRT3 in oral cancer. SIRT7 loss was observed in oral cancer cells, while its overexpression caused the suppression of oral cancer cells proliferation, migration, and invasiveness. The role of other SIRTs in oral cancer was studied meagerly or reports not available. To date, only the roles of SIRT1, SIRT3, and SIRT7 have been reported in oral malignancies. Therefore, understanding the regulatory mechanisms employed by sirtuins to modulate oral cancer is important for developing potential anti-cancer therapeutic strategies.

show abstract

Section: Sirt3 In Oral Cancermentioning

confidence: 91%

Section: Sirtuins: Types Location and Functionsmentioning

confidence: 99%

Section: Sirt1 In Oral Cancermentioning

confidence: 99%

See 1 more Smart Citation

The ambiguous role of sirtuins in head and neck squamous cell carcinoma

et al. 2021

View full text Add to dashboard Cite

show abstract

“…In another study ( Suk et al, 2019 ), a benzimidazole derivative carrying a pyrrolidine side chain ( 282) significantly suppressed sorafenib-resistant cell lines growth in xenograft model by inhibiting the phosphorylation of AKT, p70S6 and the downstream molecule RPS6, has unlocked another milestone in the treatment of hepatocellular carcinoma. Yeong et al ( Yeong et al, 2019 ) synthesized several new benzimidazole derivatives 283–287 and screened them against sirtuin cancer lines (SIRT1, SIRT2, and SIRT3). Among them, compound 284 elicited significant inhibition of SIRT1-3 compared to tenovin-6 (IC 50 (mean ± SD, µM): 7.7 ± 1.4 vs. 42.10, 5.6 ± 1.3 vs. 25.6, and 9.8 ± 2.0 vs. 82.65).…”

Section: Biological Activitiesmentioning

confidence: 99%

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

et al. 2021

View full text Add to dashboard Cite

Nowadays, nitrogenous heterocyclic molecules have attracted a great deal of interest among medicinal chemists. Among these potential heterocyclic drugs, benzimidazole scaffolds are considerably prevalent. Due to their isostructural pharmacophore of naturally occurring active biomolecules, benzimidazole derivatives have significant importance as chemotherapeutic agents in diverse clinical conditions. Researchers have synthesized plenty of benzimidazole derivatives in the last decades, amidst a large share of these compounds exerted excellent bioactivity against many ailments with outstanding bioavailability, safety, and stability profiles. In this comprehensive review, we have summarized the bioactivity of the benzimidazole derivatives reported in recent literature (2012–2021) with their available structure-activity relationship. Compounds bearing benzimidazole nucleus possess broad-spectrum pharmacological properties ranging from common antibacterial effects to the world’s most virulent diseases. Several promising therapeutic candidates are undergoing human trials, and some of these are going to be approved for clinical use. However, notable challenges, such as drug resistance, costly and tedious synthetic methods, little structural information of receptors, lack of advanced software, and so on, are still viable to be overcome for further research.

show abstract

“…Over the years, benzimidazole and its derivatives have been extensively studied in the pharmaceutical field for a wide range of pharmacological activities, which are useful for drug development. Some of the pharmacological activities which have been reported include anti‐cancer, analgesic, anti‐histamine, anti‐inflammatory, anti‐acetylcholinesterase, anti‐fungal, anti‐tubercular, anti‐viral, anti‐malarial and anti‐protozoal [1–12] . Some benzimidazole‐based drugs which have been marketed are as shown in Figure 1.…”

Section: Introductionmentioning

confidence: 99%

Benzimidazoles in Drug Discovery: A Patent Review

Law

Yoon

2021

ChemMedChem

Self Cite

View full text Add to dashboard Cite

Benzimidazole is a heterocyclic ring system that has been widely studied in the pharmaceutical field. For the past decade, numerous benzimidazole derivatives have been synthesized and evaluated for their wide range of pharmacological activities, which are beneficial for drug development. This article presents the biological effects of benzimidazole derivatives in each invention from 2015 to 2020. Two patent databases, Google Patents and Lens, were used to locate relevant granted patent applications. Specifically, this review delineates the role of patented benzimidazoles from a disease‐centric perspective and examines the mechanisms of action of these compounds in related diseases. Most of the benzimidazoles have shown good activities against various target proteins. Whilst several of them have progressed into clinical trials, most patents presented novel therapeutic approaches for respective target diseases. Hence, their potential in being developed into clinical drugs are also discussed.

show abstract

Sirtuin inhibition and anti-cancer activities of ethyl 2-benzimidazole-5-carboxylate derivatives

Abstract: Sirtuin inhibitor potently inhibits the proliferation of H103 cancer cells.

Cited by 15 publications

References 27 publications

The ambiguous role of sirtuins in head and neck squamous cell carcinoma

The ambiguous role of sirtuins in head and neck squamous cell carcinoma

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

Benzimidazoles in Drug Discovery: A Patent Review

Contact Info

Product

Resources

About