Ethenesulfonyl fluoride derivatives as telomerase inhibitors: structure-based design, SAR, and anticancer evaluation <i>in vitro</i>

Chen, Xing; Zha, Gao‐Feng; Wang, Jie Quan; Liu, Xinhua

doi:10.1080/14756366.2018.1484735

Cited by 23 publications

(11 citation statements)

References 24 publications

(13 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A structure-based design study of ethenesulfonyl fluoride derivatives, including certain 2-(hetero) arylethenesulfonyl fluoride and 1,3-dienylsulfonyl fluoride derivatives, indicates another group of chemical compounds that may be used as synthetic telomerase inhibitors and by extension in anti-cancer therapy. Some of these compounds exhibit potent inhibitory activities against telomerase though interaction with hTERT, as indicated by the modified TRAP assay ( 20 ).…”

Section: Resultsmentioning

confidence: 99%

Τelomerase inhibitors and activators in aging and cancer: A systematic review

et al. 2022

View full text Add to dashboard Cite

The main aim of the present systematic review was to summarize the most frequently used telomerase regulators with an impact on aging and cancer that are referred to in in vitro and in vivo studies. For this purpose, a systematic review of the available literature on telomerase regulators referred to in articles from PubMed and Scopus libraries published from 2002 to 2021 and in accordance with PriSMa 2020 criteria, was conducted. articles were included if they met the following criteria: They referred to telomerase modulators in aging and in cancer and were in vitro and/or in vivo studies, while studies that did not provide sufficient data or studies not written in english were excluded. in the present systematic review, 54 publications were included, of which 29 were full-text published studies, 11 were full-text reviews, 10 structure-based design studies and 4 abstracts are reported in this review. Telomerase regulators were then categorized as synthetic direct telomerase inhibitors, synthetic indirect telomerase inhibitors, synthetic telomerase activators, natural direct telomerase activators, natural telomerase inhibitors and natural indirect telomerase activators, according to their origin and their activity. on the whole, as demonstrated herein, telomerase regulators appear to be promising treatment agents in various age-related diseases. However, further in vivo and in vitro studies need to be performed in order to clarify the potentiality of telomerase as a therapeutic target.

show abstract

Section: Resultsmentioning

confidence: 99%

Τelomerase inhibitors and activators in aging and cancer: A systematic review

et al. 2022

View full text Add to dashboard Cite

show abstract

“…In 2018, a total of 82 ethenesulfonyl fluorides were screened as potential human telomerase inhibitors by Liu and coworkers. 61 The experimental results demonstrated that compounds 28c, 28d and 28e possess potent inhibitory activity against telomerase. A molecular docking experiment showed that the ethenesulfonyl fluoride fragment could be well aligned with the active site of hTERT ( Figure 3).…”

Section: Short Review Syn Thesismentioning

confidence: 94%

Ethenesulfonyl Fluoride (ESF) and Its Derivatives in SuFEx Click Chemistry and More

et al. 2019

View full text Add to dashboard Cite

The sulfur(VI) fluoride exchange reaction (SuFEx), developed by Sharpless and co-workers in 2014, is a new category of click reaction that creates molecular connections with absolute reliability and unprecedented efficiency through a sulfur(VI) hub. Ethenesulfonyl fluoride (ESF), as one of the most important sulfur(VI) hubs, exhibits extraordinary reactivity in SuFEx click chemistry and organic synthesis. This review summarizes the chemical properties and applications of ESF in click chemistry, organic chemistry, materials science, medicinal chemistry and in many other fields related to organic synthesis.1 Introduction2 Chemical Transformations of ESF3 Chemical Transformations of 2-Arylethenesulfonyl Fluorides4 Novel SuFEx Reagents Derived from ESF5 Applications of ESF Derivatives in Medicinal Chemistry6 Applications of ESF Derivatives in Materials Science7 Conclusion

show abstract

“…Among them, 3‐(3,5‐dichlorophenoxy)‐nitrostyrene ( 28 ) may inhibit hTERT via binding to a site distinct from the active site. Ethenesulfonyl fluoride derivatives containing a styrene structure showed telomerase inhibition, wherein compounds 29 , 30 , and 31 showed inhibitory activities with IC 50 of 0.71, 0.81, and 0.97 mM, respectively …”

Section: Small Molecule Inhibitorsmentioning

confidence: 99%

Therapeutic strategies for targeting telomerase in cancer

Chen

Tang

Shi

et al. 2019

Medicinal Research Reviews

Self Cite

View full text Add to dashboard Cite

Telomere and telomerase play important roles in abnormal cell proliferation, metastasis, stem cell maintenance, and immortalization in various cancers. Therefore, designing of drugs targeting telomerase and telomere is of great significance. Over the past two decades, considerable knowledge regarding telomere and telomerase has been accumulated, which provides theoretical support for the design of therapeutic strategies such as telomere elongation. Therefore, the development of telomere‐based therapies such as nucleoside analogs, non‐nucleoside small molecules, antisense technology, ribozymes, and dominant negative human telomerase reverse transcriptase are being prioritized for eradicating a majority of tumors. While the benefits of telomere‐based therapies are obvious, there is a need to address the limitations of various therapeutic strategies to improve the possibility of clinical applications. In this study, current knowledge of telomere and telomerase is discussed, and therapeutic strategies based on recent research are reviewed.

show abstract

Ethenesulfonyl fluoride derivatives as telomerase inhibitors: structure-based design, SAR, and anticancer evaluation in vitro

Cited by 23 publications

References 24 publications

Τelomerase inhibitors and activators in aging and cancer: A systematic review

Τelomerase inhibitors and activators in aging and cancer: A systematic review

Ethenesulfonyl Fluoride (ESF) and Its Derivatives in SuFEx Click Chemistry and More

Therapeutic strategies for targeting telomerase in cancer

Contact Info

Product

Resources

About