Synthesis of Betulinic Acid Derivatives with Modified A-Rings and their Application as Potential Drug Candidates

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15110%2F18%3A73590478" target="_blank" >RIV/61989592:15110/18:73590478 - isvavai.cz</a>

Výsledek na webu

<a href="http://dx.doi.org/10.1002/ajoc.201800163" target="_blank" >http://dx.doi.org/10.1002/ajoc.201800163</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1002/ajoc.201800163" target="_blank" >10.1002/ajoc.201800163</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Synthesis of Betulinic Acid Derivatives with Modified A-Rings and their Application as Potential Drug Candidates

Popis výsledku v původním jazyce

This Focus Review summarizes recent advances in the synthesis of betulinic acid derivatives with modified A-rings. It also focuses on their application as potential therapeutic agents for the treatment of cancer and other diseases. Betulinic acid (BA) exhibits therapeutically interesting biological properties, including antitumor, anti-HIV, antiprotozoal, and hepato- or nephroprotective activity; however, its clinical use has been severely limited by its higher IC50 value and worse pharmacological parameters than the currently used drugs. On the other hand, semisynthetic analogues of BA are much better suited for potential clinical use. Among these analogues, compounds that contain a modified A-ring are the most promising. We hope that this Focus Review will serve as a guide for the synthesis of new BA derivatives with applications as drug candidates. A general audience may also find this Focus Review interesting, because it describes the structural motifs that are responsible for the observed bioactivities.

Název v anglickém jazyce

Synthesis of Betulinic Acid Derivatives with Modified A-Rings and their Application as Potential Drug Candidates

Popis výsledku anglicky

This Focus Review summarizes recent advances in the synthesis of betulinic acid derivatives with modified A-rings. It also focuses on their application as potential therapeutic agents for the treatment of cancer and other diseases. Betulinic acid (BA) exhibits therapeutically interesting biological properties, including antitumor, anti-HIV, antiprotozoal, and hepato- or nephroprotective activity; however, its clinical use has been severely limited by its higher IC50 value and worse pharmacological parameters than the currently used drugs. On the other hand, semisynthetic analogues of BA are much better suited for potential clinical use. Among these analogues, compounds that contain a modified A-ring are the most promising. We hope that this Focus Review will serve as a guide for the synthesis of new BA derivatives with applications as drug candidates. A general audience may also find this Focus Review interesting, because it describes the structural motifs that are responsible for the observed bioactivities.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10401 - Organic chemistry

Projekt

<a href="/cs/project/LO1304" target="_blank" >LO1304: Podpora udržitelnosti Ústavu molekulární a translační medicíny</a><br>

Návaznosti

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

Rok uplatnění

2018

Kód důvěrnosti údajů

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

Název periodika

Asian Journal of Organic Chemistry

ISSN

2193-5807

e-ISSN

—

Svazek periodika

7

Číslo periodika v rámci svazku

8

Stát vydavatele periodika

DE - Spolková republika Německo

Počet stran výsledku

19

Strana od-do

1542-1560

Kód UT WoS článku

000441415100008

EID výsledku v databázi Scopus

2-s2.0-85051420974