Synthesis and Antiviral Activities of Synthetic Glutarimide Derivatives

Ji, Xiangming; Zhong, Zhao-jin; Xue, Si-tu; Meng, Sheng; He, Weiying; Gao, Rongmei; Li, Yuhuan; Li, Zhuorong

doi:10.1248/cpb.58.1436

Cited by 14 publications

(9 citation statements)

References 28 publications

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“…The scientific interest for CHX has, however, declined because of its toxicity level, which is too high for the application in humans and because no CHX analogues showed any improvement in activity or toxicity [127,128]. Recently, cycloheximide was derivatized as a fluorescent probe for protein synthesis imaging [129], and also tested as inhibitor of FKBP12 [130] or as an antiviral [131]. These studies have shown that most of the molecular features are essential to maintain its activity ( Figure 6).…”

Section: Cryo-em-based Drug Design Of Cycloheximidementioning

confidence: 99%

Targeting the Human 80S Ribosome in Cancer: From Structure to Function and Drug Design for Innovative Adjuvant Therapeutic Strategies

Gilles

Fréchin

Natchiar

et al. 2020

Cells

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The human 80S ribosome is the cellular nucleoprotein nanomachine in charge of protein synthesis that is profoundly affected during cancer transformation by oncogenic proteins and provides cancerous proliferating cells with proteins and therefore biomass. Indeed, cancer is associated with an increase in ribosome biogenesis and mutations in several ribosomal proteins genes are found in ribosomopathies, which are congenital diseases that display an elevated risk of cancer. Ribosomes and their biogenesis therefore represent attractive anti-cancer targets and several strategies are being developed to identify efficient and specific drugs. Homoharringtonine (HHT) is the only direct ribosome inhibitor currently used in clinics for cancer treatments, although many classical chemotherapeutic drugs also appear to impact on protein synthesis. Here we review the role of the human ribosome as a medical target in cancer, and how functional and structural analysis combined with chemical synthesis of new inhibitors can synergize. The possible existence of oncoribosomes is also discussed. The emerging idea is that targeting the human ribosome could not only allow the interference with cancer cell addiction towards protein synthesis and possibly induce their death but may also be highly valuable to decrease the levels of oncogenic proteins that display a high turnover rate (MYC, MCL1). Cryo-electron microscopy (cryo-EM) is an advanced method that allows the visualization of human ribosome complexes with factors and bound inhibitors to improve our understanding of their functioning mechanisms mode. Cryo-EM structures could greatly assist the foundation phase of a novel drug-design strategy. One goal would be to identify new specific and active molecules targeting the ribosome in cancer such as derivatives of cycloheximide, a well-known ribosome inhibitor.

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Section: Cryo-em-based Drug Design Of Cycloheximidementioning

confidence: 99%

Targeting the Human 80S Ribosome in Cancer: From Structure to Function and Drug Design for Innovative Adjuvant Therapeutic Strategies

Gilles

Fréchin

Natchiar

et al. 2020

Cells

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“…Cycloheximide can be useful to the host plant as an antifungal and antiviral compound (Ji et al 2010). …”

Section: Discussionmentioning

confidence: 99%

Endophytic Streptomyces in the traditional medicinal plant Arnica montana L.: secondary metabolites and biological activity

Wardecki

Brötz

Ford

et al. 2015

Antonie van Leeuwenhoek

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“…Furthermore, the applications of these chemical treatments have some worrying effects on human health and ecosystems. Examples of this would be toxicity to organisms and the suppression of beneficial microbes [9,[11][12][13]. Nowadays, raising concerns about the high cost of chemicals, and the environmental problems they are associated with, have encouraged researchers to seek alternative strategies for BSR suppression.…”

Section: Introductionmentioning

confidence: 99%

New Antimicrobial Phenyl Alkenoic Acids Isolated from an Oil Palm Rhizosphere-Associated Actinomycete, Streptomyces palmae CMU-AB204T

et al. 2020

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Basal stem rot (BSR), or Ganoderma rot disease, is the most serious disease associated with the oil palm plant of Southeast Asian countries. A basidiomycetous fungus, Ganoderma boninense, is the causative microbe of this disease. To control BSR in oil palm plantations, biological control agents are gaining attention as a major alternative to chemical fungicides. In the course of searching for effective actinomycetes as potential biological control agents for BSR, Streptomyces palmae CMU-AB204T was isolated from oil palm rhizosphere soil collected on the campus of Chiang Mai University. The culture broth of this strain showed significant antimicrobial activities against several bacteria and phytopathogenic fungi including G. boninense. Antifungal and antibacterial compounds were isolated by antimicrobial activity-guided purification using chromatographic methods. Their structures were elucidated by spectroscopic techniques, including Nuclear Magnetic Resonance (NMR), Mass Spectrometry (MS), Ultraviolet (UV), and Infrared (IR) analyses. The current study isolated new phenyl alkenoic acids 1–6 and three known compounds, anguinomycin A (7), leptomycin A (8), and actinopyrone A (9) as antimicrobial agents. Compounds 1 and 2 displayed broad antifungal activity, though they did not show antibacterial activity. Compounds 3 and 4 revealed a strong antibacterial activity against both Gram-positive and Gram-negative bacteria including the phytopathogenic strain Xanthomonas campestris pv. oryzae. Compounds 7–9 displayed antifungal activity against Ganoderma. Thus, the antifungal compounds obtained in this study may play a role in protecting oil palm plants from Ganoderma infection with the strain S. palmae CMU-AB204T.

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Synthesis and Antiviral Activities of Synthetic Glutarimide Derivatives

Cited by 14 publications

References 28 publications

Targeting the Human 80S Ribosome in Cancer: From Structure to Function and Drug Design for Innovative Adjuvant Therapeutic Strategies

Targeting the Human 80S Ribosome in Cancer: From Structure to Function and Drug Design for Innovative Adjuvant Therapeutic Strategies

Endophytic Streptomyces in the traditional medicinal plant Arnica montana L.: secondary metabolites and biological activity

New Antimicrobial Phenyl Alkenoic Acids Isolated from an Oil Palm Rhizosphere-Associated Actinomycete, Streptomyces palmae CMU-AB204T

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