Discovery of an indole-substituted furanone with tubulin polymerization inhibition activity

Mowery, Patricia; Filkorn, Madison M.; Hurysz, Brianna; Kwansare, Deborah O.; Lafferty, Megan M.; McFadden, Marissa A.; Neerukonda, Namita D.; Patel, Roslyn R.; Pierce, Kelsey; Sockett, Kaitlynn A.; Truax, Nathanyal J.; Webster, Nathan R.; Pelkey, Erin T.

doi:10.1016/j.bmcl.2021.127991

Cited by 9 publications

(3 citation statements)

References 72 publications

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“…The stabilization or destabilization of microtubule polymerization was estimated using the in vitro tubulin polymerization assay kit (Catalog no. BK0066P; Cytoskeleton, Inc., Denver, CO, USA).…”

Section: Methodsmentioning

confidence: 99%

Appraisal of Chitosan-Gum Arabic-Coated Bipolymeric Nanocarriers for Efficient Dye Removal and Eradication of the Plant Pathogen Botrytis cinerea

Raj

Raorane

Lee

2021

ACS Appl. Mater. Interfaces

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The treatment of textile wastewater comprising many dyes as contaminants endures an essential task for environmental remediation. In addition, combating antifungal multidrug resistance (MDR) is an intimidating task, specifically owing to the limited options of alternative drugs with multitarget drug mechanisms. Incorporating natural polymeric biomaterials for drug delivery provides desirable properties for drug molecules, effectively eradicating MDR fungal growth. The current study fabricated the bipolymeric drug delivery system using chitosan-gum arabic-coated liposome 5ID nanoparticles (CS-GA-5ID-LP-NPs). This study focused on improving the solubility and sustained release profile of 5I-1H-indole (5ID). These NPs were characterized and tested mechanically as a dye adsorbent as well as their antifungal potencies against the plant pathogen, Botrytis cinerea. CS-GA-5ID-LP-NPs showed 71.23% congo red dye removal compared to crystal violet and phenol red from water and effectively had an antifungal effect on B. cinerea at 25 μg/mL MIC concentrations. The mechanism of the inhibition of B. cinerea via CS-GA-5ID-LP-NPs was attributed to stabilized microtubule polymerization in silico and in vitro. This study opens a new avenue for designing polymeric NPs as adsorbents and antifungal agents for environmental and agriculture remediation.

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Section: Methodsmentioning

confidence: 99%

Appraisal of Chitosan-Gum Arabic-Coated Bipolymeric Nanocarriers for Efficient Dye Removal and Eradication of the Plant Pathogen Botrytis cinerea

Raj

Raorane

Lee

2021

ACS Appl. Mater. Interfaces

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“…Meanwhile, St.28 ( Figure 7 ) with indole-amino-pyrazolyl derivatives was synthesized and inhibited tubulin polymerization with IC 50 values of 0.28 μM [ 90 ]. In new research on a indole-furanone hybrid, derivatives were synthesized and developed as anti-tubulin derivatives; the most potent compound, St.29 ( Figure 7 ), has anticancer and antimitotic potency at the micromolar level [ 91 ]. In another recent work, the authors developed and synthesized an indole-heterocycle hybrid like the furan ring, and these structures showed potent antiproliferative activities.…”

Section: Indole Analoguesmentioning

confidence: 99%

“…The indole-amide class was considered one of the main classes of indole derivatives with anticancer and/or anti-tubulin activities [ 22 , 91 , 93 ]. A series of indole-acrylamide was synthesized and developed as anti-tubulin inhibitors, and St.32 ( Figure 7 ) showed inhibitory activities of tubulin polymerization.…”

Section: Indole Analoguesmentioning

confidence: 99%

Recent Advances of Tubulin Inhibitors Targeting the Colchicine Binding Site for Cancer Therapy

Hawash

2022

Biomolecules

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Cancer accounts for numerous deaths each year, and it is one of the most common causes of death worldwide, despite many breakthroughs in the discovery of novel anticancer candidates. Each new year the FDA approves the use of new drugs for cancer treatments. In the last years, the biological targets of anticancer agents have started to be clearer and one of these main targets is tubulin protein; this protein plays an essential role in cell division, as well as in intracellular transportation. The inhibition of microtubule formation by targeting tubulin protein induces cell death by apoptosis. In the last years, numerous novel structures were designed and synthesized to target tubulin, and this can be achieved by inhibiting the polymerization or depolymerization of the microtubules. In this review article, recent novel compounds that have antiproliferation activities against a panel of cancer cell lines that target tubulin are explored in detail. This review article emphasizes the recent developments of tubulin inhibitors, with insights into their antiproliferative and anti-tubulin activities. A full literature review shows that tubulin inhibitors are associated with properties in the inhibition of cancer cell line viability, inducing apoptosis, and good binding interaction with the colchicine binding site of tubulin. Furthermore, some drugs, such as cabazitaxel and fosbretabulin, have been approved by FDA in the last three years as tubulin inhibitors. The design and development of efficient tubulin inhibitors is progressively becoming a credible solution in treating many species of cancers.

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Discovery of indole-3-acetic acid derivatives containing 1,3,4-thiadiazole thioether and amide moieties as novel antibacterial agents

Tang,

Shao,

et al. 2024

Chem Heterocycl Comp

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Discovery of an indole-substituted furanone with tubulin polymerization inhibition activity

Cited by 9 publications

References 72 publications

Appraisal of Chitosan-Gum Arabic-Coated Bipolymeric Nanocarriers for Efficient Dye Removal and Eradication of the Plant Pathogen Botrytis cinerea

Appraisal of Chitosan-Gum Arabic-Coated Bipolymeric Nanocarriers for Efficient Dye Removal and Eradication of the Plant Pathogen Botrytis cinerea

Recent Advances of Tubulin Inhibitors Targeting the Colchicine Binding Site for Cancer Therapy

Discovery of indole-3-acetic acid derivatives containing 1,3,4-thiadiazole thioether and amide moieties as novel antibacterial agents

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