Triterpenoid-PEG Ribbons Targeting Selectivity in Pharmacological Effects

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22330%2F21%3A43922244" target="_blank" >RIV/60461373:22330/21:43922244 - isvavai.cz</a>

Alternative codes found

RIV/61389030:_____/21:00549087 RIV/61388963:_____/21:00549087 RIV/61989592:15310/21:73610839

Result on the web

<a href="https://www.mdpi.com/2227-9059/9/8/951" target="_blank" >https://www.mdpi.com/2227-9059/9/8/951</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/biomedicines9080951" target="_blank" >10.3390/biomedicines9080951</a>

Result language

angličtina

Original language name

Triterpenoid-PEG Ribbons Targeting Selectivity in Pharmacological Effects

Original language description

(1) Background: To compare the effect of selected triterpenoids with their structurally resembling derivatives, designing of the molecular ribbons was targeted to develop compounds with selectivity in their pharmacological effects. (2) Methods: In the synthetic procedures, Huisgen 1,3‐ dipolar cycloaddition was applied as a key synthetic step for introducing a 1,2,3‐triazole ring as a part of a junction unit in the molecular ribbons. (3) Results: The antimicrobial activity, antiviral activity, and cytotoxicity of the prepared compounds were studied. Most of the molecular ribbons showed antimicrobial activity, especially on Staphylococcus aureus, Pseudomonas aeruginosa, and Enterococcus faecalis, with a 50–90% inhibition effect (c = 25 μg∙mL−1). No target compound was effective against HSV‐1, but 8a displayed activity against HIV‐1 (EC50 = 50.6 ± 7.8 μM). Cytotoxicity was tested on several cancer cell lines, and 6d showed cytotoxicity in the malignant melanoma cancer cell line (G‐361; IC50 = 20.0 ± 0.6 μM). Physicochemical characteristics of the prepared compounds were investigated, namely a formation of supramolecular gels and a self‐assembly potential in general, with positive results achieved with several target compounds. (4) Conclusions: Several compounds of a series of triterpenoid molecular ribbons showed better pharmacological profiles than the parent compounds and displayed certain selectivity in their effects. © 2021 by the authors. Licensee MDPI, Basel, Switzerland.

Czech name

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Czech description

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Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

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OECD FORD branch

10609 - Biochemical research methods

Project

Result was created during the realization of more than one project. More information in the Projects tab.

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year

2021

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Biomedicines

ISSN

2227-9059

e-ISSN

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Volume of the periodical

9

Issue of the periodical within the volume

8

Country of publishing house

CH - SWITZERLAND

Number of pages

14

Pages from-to

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UT code for WoS article

000688878800001

EID of the result in the Scopus database

2-s2.0-85112313481